Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44417940 81282 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81282 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
137644041 157903 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157903 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
137644041 157903 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157903 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
10150552 81181 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81181 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417944 141278 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141278 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417894 80172 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80172 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417921 80713 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 80713 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417925 81052 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81052 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417875 80382 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80382 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417823 165219 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165219 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141236 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141236 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
44207909 16520 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16520 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16520 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16520 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
15133403 204627 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 204627 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018999 80707 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 80707 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018957 82030 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82030 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141028 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141028 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417998 81983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 81983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018944 81796 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 81796 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417962 81674 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 81674 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417846 81687 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 81687 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25110804 95046 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95046 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44454966 154887 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 154887 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44417917 81684 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 81684 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418009 81451 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81451 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 81888 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 81888 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44455444 94602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 94602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455414 96968 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 96968 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455417 97012 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 97012 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
24952417 91084 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91084 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952419 91094 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91094 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417867 140981 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 140981 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018896 141162 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141162 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
10150954 141015 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141015 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24808474 91091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417956 96203 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96203 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417947 140979 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 140979 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
10310316 80708 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 80708 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24952765 91096 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91096 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10173787 82026 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82026 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018932 79896 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 79896 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417843 81549 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81549 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417886 141166 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141166 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 168453 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 168453 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455368 95186 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95186 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952418 91086 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91086 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135478 91088 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91088 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135482 91092 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91092 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135474 91093 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91093 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
22018997 141176 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141176 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417992 82045 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82045 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10173726 80433 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80433 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417857 141124 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141124 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150955 80507 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80507 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417888 79995 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 79995 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417999 81794 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 81794 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018856 80195 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80195 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
44417995 82029 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82029 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417847 82023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417821 80147 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80147 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
10126754 81145 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81145 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455443 95267 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95267 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952056 91087 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91087 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141354 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141354 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018945 141191 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141191 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417966 160971 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 160971 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018914 80503 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80503 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
59135486 91090 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91090 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417975 141328 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141328 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141265 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141265 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417838 81185 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81185 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417877 80725 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 80725 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135492 91095 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91095 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417911 82027 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82027 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417915 140857 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 140857 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
24952055 91089 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91089 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141354 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141354 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417845 141354 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141354 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417864 79880 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 79880 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417979 81734 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 81734 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417948 141217 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141217 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44455367 95185 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95185 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
59135471 91082 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91082 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417973 140943 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 140943 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417844 141055 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141055 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417982 82100 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82100 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417848 141090 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141090 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417832 141220 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141220 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417976 165389 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165389 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417959 81383 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81383 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018964 141138 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141138 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44418003 82056 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82056 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417873 81047 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81047 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44418002 82153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
9799244 80173 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80173 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141285 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141285 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417856 80428 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80428 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
11994411 989 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
1306 989 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
CHEMBL214523 989 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
4033 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
9826520 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
CHEMBL214957 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
4033 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
9826520 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
CHEMBL214957 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
10004545 74603 4 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11995648 81986 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
CHEMBL217269 81986 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
11994912 82478 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
CHEMBL218077 82478 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
10004545 74603 4 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10004545 74603 4 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11994412 141179 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
CHEMBL385690 141179 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
11993893 141291 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
CHEMBL386349 141291 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
11995024 140902 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL384133 140902 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
11995242 80405 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
CHEMBL215235 80405 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
44416336 79653 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
CHEMBL213008 79653 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
44442095 93866 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 93866 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11994413 80108 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
CHEMBL214806 80108 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
11994784 81880 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL217178 81880 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
11994786 82180 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
CHEMBL217887 82180 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
10004545 74603 4 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44416314 79555 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212657 79555 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11994913 80142 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
CHEMBL214871 80142 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
11994659 81139 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
CHEMBL216117 81139 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
11993894 82151 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217843 82151 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
11994780 82098 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
CHEMBL217733 82098 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
11995244 80163 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214944 80163 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
44416857 79832 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
CHEMBL213813 79832 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
11553871 80705 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL215643 80705 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
44416316 168720 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL441368 168720 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416837 141008 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384724 141008 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
10225681 79928 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214276 79928 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414475 77721 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 77721 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44417150 79823 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213766 79823 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416976 81064 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL216005 81064 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
23027411 196843 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 196843 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44430471 86378 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86378 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430460 86798 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 86798 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
44430463 148867 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 148867 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
70688018 74494 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74494 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436085 74539 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74539 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44394824 123749 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 123749 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
10025637 65253 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65253 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44416751 81708 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
CHEMBL216649 81708 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
44416350 141419 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL387195 141419 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485029 196816 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577714 196816 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
54581468 60261 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760068 60261 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
45267576 194957 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 194957 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
70687479 73163 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73163 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57402044 68502 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922251 68502 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
23532179 68504 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922253 68504 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57395050 68514 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68514 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44394800 121842 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 121842 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123114 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123114 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 130930 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 130930 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11189610 165224 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165224 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
20817821 76506 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76506 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
23120540 194465 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 194465 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031907 138596 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786923 138596 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
57398576 68500 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922249 68500 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57402045 68503 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922252 68503 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
10202381 68516 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68516 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44418006 81998 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217349 81998 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973799 82050 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82050 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11188955 80057 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80057 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
3114950 37536 29 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37536 29 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
54586331 60260 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760065 60260 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
11526309 188629 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 188629 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
44417983 81748 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216935 81748 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70689520 73119 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73119 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11837128 71786 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 71786 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
44562404 176390 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176390 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
44410878 77754 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 77754 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
44592257 178413 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470840 178413 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
58062385 125356 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
CHEMBL3648387 125356 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
4062524 32406 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
CHEMBL1412874 32406 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
46846317 58841 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
CHEMBL1699198 58841 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
46846319 58896 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
CHEMBL1701679 58896 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
24856242 35075 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
CHEMBL1436519 35075 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
49866089 16069 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16069 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44405481 71506 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71506 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691720 73206 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73206 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
23120586 195062 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 195062 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
2729098 80084 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80084 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
11563383 70171 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70171 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
52917998 60308 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60308 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430477 86790 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 86790 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430476 151774 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 151774 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
23593464 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436117 74544 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74544 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
53324076 56415 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56415 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
21108056 67738 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 67738 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391028 67743 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67743 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9910346 64401 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64401 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10070016 71119 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
CHEMBL196208 71119 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
11775399 63030 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63030 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11495754 71588 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71588 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57404360 72800 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011534 72800 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
49865653 15866 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 15866 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865678 15884 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 15884 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
10183297 92880 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 92880 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
44394909 66699 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 66699 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44394856 65803 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 65803 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
46850893 59411 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
CHEMBL1723963 59411 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
46172926 59026 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1706758 59026 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46861572 125345 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
CHEMBL3648376 125345 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
46172933 59551 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
CHEMBL1729376 59551 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
3247171 23126 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
CHEMBL1332346 23126 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
23603500 21627 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
CHEMBL1319565 21627 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
49866035 16054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417961 81665 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216564 81665 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394866 123830 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 123830 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
16438224 52014 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
CHEMBL1589201 52014 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
54580459 60259 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760063 60259 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
46846318 59329 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1720892 59329 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
58062375 125363 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
CHEMBL3648394 125363 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
44394807 65886 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 65886 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44405646 96425 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96425 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
70691649 73108 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73108 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
58062307 125349 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
CHEMBL3648380 125349 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
11562129 70733 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70733 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562442 178610 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 178610 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
58062320 125344 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648375 125344 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
46188959 121248 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589135 121248 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
44442151 93572 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 93572 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
2810388 42253 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
CHEMBL1499675 42253 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
44414520 79861 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 79861 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
11547011 141082 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141082 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
11610423 165466 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 165466 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
52918016 60322 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60322 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436082 74541 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74541 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689612 73257 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73257 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11635674 200164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
11496313 71968 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71968 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416956 79835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213824 79835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416995 82679 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL218186 82679 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
44416348 80823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215862 80823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414589 79754 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 79754 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45484995 196842 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 196842 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11713742 93130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11570031 73151 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73151 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44397202 66888 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 66888 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
127032787 138628 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787237 138628 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
10319824 66746 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 66746 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
46835812 59219 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1716158 59219 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
5810215 26199 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
CHEMBL1359426 26199 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
45269336 194308 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 194308 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
58062364 125347 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
CHEMBL3648378 125347 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
5091342 51521 6 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
CHEMBL1585038 51521 6 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
45273642 194781 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 194781 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44562545 188514 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 188514 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
46835786 59279 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
CHEMBL1718965 59279 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
58062388 125342 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
CHEMBL3648373 125342 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
44416363 79965 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214427 79965 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
1479656 59475 13 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
CHEMBL1726382 59475 13 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
24856245 45870 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
CHEMBL1533829 45870 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
2982342 54872 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1342885 54872 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1617311 54872 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
11995644 81956 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217228 81956 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416297 96530 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL266415 96530 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44394592 65431 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65431 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
45382326 59525 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1728485 59525 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
16191617 50463 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
CHEMBL1576145 50463 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
44442153 93613 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 93613 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
46835820 59501 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1727473 59501 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
2386953 54981 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1339438 54981 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1618129 54981 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
23027035 196870 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 196870 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
11583049 141416 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141416 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
44430459 86736 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 86736 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
16718619 121251 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589154 121251 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
70691736 73254 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73254 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693807 73255 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73255 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10369833 92135 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92135 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
44414481 138371 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138371 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54580457 60255 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60255 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10456385 91708 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 91708 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
44394606 66917 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 66917 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397008 66568 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66568 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
16756405 92435 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92435 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
9955811 65840 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 65840 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
10377822 126303 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126303 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
135519896 71754 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
CHEMBL1977747 71754 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
90666255 108877 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 108877 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
3338232 39204 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
CHEMBL1471999 39204 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
22254604 123358 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123358 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
952248 46295 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
CHEMBL1537947 46295 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
46846336 59471 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1726190 59471 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
11592099 93069 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93069 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
44410904 171890 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171890 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11974131 141454 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141454 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
90666251 108873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 108873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45382325 59145 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
CHEMBL1712328 59145 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
44405431 71607 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71607 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
46892535 125341 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
CHEMBL3648372 125341 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
54579973 60318 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60318 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436120 74530 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74530 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
70693734 73130 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73130 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687551 73270 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73270 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70691738 73275 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73275 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
24857598 18929 12 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 18929 12 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11655872 71373 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71373 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
10027853 71518 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71518 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
50908737 18945 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 18945 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
54587368 60264 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760077 60264 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
57404359 72797 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011528 72797 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
127033672 138492 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785819 138492 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690365 137647 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137647 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
16755969 91883 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 91883 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394764 122653 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 122653 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
9895868 69239 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69239 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
16756640 92846 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 92846 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
11994910 80004 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL214571 80004 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
70681198 73226 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73226 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46850887 59386 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
CHEMBL1723067 59386 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
49865868 16000 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 16000 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062381 125343 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648374 125343 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
58062316 125352 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648383 125352 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
10255474 123154 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123154 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
11510669 188710 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 188710 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70693795 73212 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73212 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45382320 59679 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
CHEMBL1734525 59679 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
70687470 73114 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73114 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865977 16042 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16042 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062334 125346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648377 125346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
58062344 125359 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
CHEMBL3648390 125359 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
70691333 77618 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77618 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
135693566 23559 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
CHEMBL1335685 23559 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
11539632 70217 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70217 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44414432 77584 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77584 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666094 108839 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 108839 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430468 91929 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 91929 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
127031622 138660 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787639 138660 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11511776 188711 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 188711 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70681213 73256 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73256 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11520239 3575 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3575 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3575 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
4219492 71093 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71093 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44417043 80960 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215932 80960 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
44417067 141460 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387438 141460 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
54584908 60315 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760242 60315 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
127031909 138622 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787166 138622 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
70685336 73107 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73107 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394683 66872 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 66872 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46850894 59048 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1707830 59048 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
2827417 54223 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
CHEMBL1609915 54223 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
3732471 38652 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
CHEMBL1467280 38652 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
54585833 60298 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760222 60298 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
54585862 60306 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760230 60306 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
49865654 15867 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 15867 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70689526 73160 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73160 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
1129890 55865 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1578660 55865 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1625981 55865 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
70681116 73116 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73116 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44416255 79639 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212963 79639 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
2766793 49808 12 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
CHEMBL1569862 49808 12 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
4439874 51212 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
CHEMBL1582511 51212 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
46835815 59007 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
CHEMBL1705920 59007 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
2709719 26208 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
CHEMBL1359489 26208 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
23027245 195452 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 195452 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
11683903 82017 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82017 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
71226964 128659 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 128659 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11599186 73152 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73152 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
16718619 121251 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121251 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
4033 1868 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1868 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1868 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
60150483 73205 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73205 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70685409 73261 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73261 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11583744 71380 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71380 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10005009 165823 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165823 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54586330 60256 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760060 60256 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
11374857 79809 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 79809 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
70681114 73112 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73112 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
54582960 60309 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760235 60309 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394639 66373 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66373 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948187 52597 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
CHEMBL1595687 52597 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
20854116 25220 6 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
CHEMBL1350024 25220 6 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
11611530 134282 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134282 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
70695853 73122 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73122 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553316 71290 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71290 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
45269335 194789 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 194789 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
11155432 82075 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82075 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
16190353 24489 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
CHEMBL1343746 24489 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
786990 51706 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
CHEMBL1586617 51706 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
11640515 80098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11640515 80098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
22254551 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254551 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
22254551 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 124524 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
17596249 33085 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
CHEMBL1418691 33085 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
10041636 122679 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 122679 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
21940008 64394 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64394 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64401 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64401 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56414 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56414 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11505089 193139 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 193139 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
70685407 73253 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73253 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
54585377 60265 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760078 60265 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54585378 60266 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760079 60266 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54582958 60302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760226 60302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70695929 73268 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73268 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394959 66874 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66874 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394907 165439 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165439 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
46172924 59306 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
CHEMBL1720022 59306 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
1479652 51452 13 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51452 13 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46172940 59285 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
CHEMBL1719118 59285 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
11974230 165459 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 165459 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
800280 46419 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
CHEMBL1539046 46419 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
58062315 125357 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
CHEMBL3648388 125357 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
22254571 66635 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66635 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
46172927 59418 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
CHEMBL1724285 59418 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
53317307 56418 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56418 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
44438741 93391 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93391 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
660602 54893 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1314041 54893 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1617460 54893 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
58062386 125360 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
CHEMBL3648391 125360 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
44417883 79954 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL214383 79954 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
89691096 138947 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138947 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
23593474 64372 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64372 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11559625 56421 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56421 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687473 73127 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73127 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685410 73264 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73264 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46933537 15887 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 15887 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417850 81245 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81245 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
57391574 68511 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922260 68511 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
57403783 68512 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922261 68512 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
46850892 59701 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1735215 59701 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
70695854 73123 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73123 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44388559 60395 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60395 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44417970 97771 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL274326 97771 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70695916 73223 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73223 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405518 139829 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 139829 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46172915 59213 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1715946 59213 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
24892611 55602 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1538063 55602 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1623531 55602 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
49865928 16019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
12005269 39977 5 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
CHEMBL1480448 39977 5 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
11560917 123534 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 123534 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44405519 72026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11995343 80014 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214604 80014 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
1314 3670 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
9865843 3670 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
CHEMBL178707 3670 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
56598528 138540 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786350 138540 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690574 137797 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137797 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
24780883 56419 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56419 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
44557554 194737 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 194737 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
70681217 73273 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73273 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11705240 132292 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132292 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416871 80086 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214733 80086 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416296 79966 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214429 79966 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
16755970 91882 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 91882 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
16756284 150954 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 150954 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
44394572 66181 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66181 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405415 72224 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72224 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
11975326 80097 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80097 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
58062298 125358 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
CHEMBL3648389 125358 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
44410944 76699 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 76699 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394855 66944 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 66944 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
135515070 20928 1 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
CHEMBL1312413 20928 1 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
11464405 80085 18 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80085 18 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
70687537 73204 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73204 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
58062333 125348 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648379 125348 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
44438748 148965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 148965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11842385 37897 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
CHEMBL1461182 37897 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
44416232 79689 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL213154 79689 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995025 168275 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
CHEMBL437914 168275 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
11993892 141085 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
CHEMBL385171 141085 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
9821717 196861 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL578049 196861 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522703 76023 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76023 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
16006978 79663 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79663 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11995347 80495 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
CHEMBL215286 80495 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
23027806 195531 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
CHEMBL568208 195531 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
18436094 74536 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74536 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994660 96105 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
CHEMBL262945 96105 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
23027679 196869 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578166 196869 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44417021 80082 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214716 80082 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416337 79963 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214416 79963 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
18436038 76021 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76021 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
11994911 141456 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
CHEMBL387419 141456 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
9932896 74178 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74178 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
57398088 67740 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67740 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9932896 74178 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74178 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
45485062 195492 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 195492 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
57521365 2577 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2577 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2577 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
44414309 138360 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138360 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL472083 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL534717 178565 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
23120512 193638 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 193638 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
24963343 72802 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 72802 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
16739324 149227 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149227 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
71226400 128661 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 128661 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 138538 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 138538 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
127031338 138542 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 138542 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
71226277 138589 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 138589 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57403784 68513 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68513 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23532181 68515 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922266 68515 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
70681214 73259 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73259 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44469273 195881 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 195881 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10436090 65874 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 65874 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394609 123367 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123367 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
44394792 124220 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124220 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
16659240 81802 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217079 81802 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
22348155 76232 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76232 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
22348261 76710 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 76710 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
22348066 165277 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165277 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
11995141 80742 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL215782 80742 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
45485004 196763 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL577259 196763 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
127033096 138649 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787492 138649 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57393331 68505 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922254 68505 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57391572 68506 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922255 68506 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
16756637 92771 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 92771 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
46835808 59116 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
CHEMBL1710711 59116 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
30979231 69183 3 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934102 69183 3 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
46846334 59204 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1715364 59204 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
3527724 50216 3 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
CHEMBL1573548 50216 3 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
54584904 60301 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760225 60301 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
11546687 81143 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81143 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
5129939 36106 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
CHEMBL1446321 36106 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
58062355 125350 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
CHEMBL3648381 125350 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
10024171 187462 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 187462 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
56597689 138636 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 138636 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11599973 193228 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 193228 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
70681216 73266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45484984 195583 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568458 195583 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
10083869 65243 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65243 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46835819 58992 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
CHEMBL1705448 58992 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
10083869 65243 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11545677 70034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417974 96595 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL266972 96595 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11974233 81730 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 81730 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
1082177 25676 5 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
CHEMBL1353612 25676 5 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
90666098 108843 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 108843 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45273659 194159 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 194159 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44394604 124530 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 124530 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
1933024 26115 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
CHEMBL1358809 26115 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
44143495 183673 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 183673 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
127030069 138578 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 138578 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597988 138623 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 138623 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317306 56411 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56411 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53325164 56423 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56423 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
57392823 67739 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 67739 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
10000146 64316 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64316 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
127033673 138569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786609 138569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
23593472 64374 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64374 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70695915 73220 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73220 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394611 123828 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 123828 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 123828 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 123828 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
54584906 60313 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760239 60313 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46172941 59250 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1717450 59250 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
675719 41602 16 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
CHEMBL1493564 41602 16 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
58062312 125351 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
CHEMBL3648382 125351 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
44394799 65922 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 65922 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
70695913 73202 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73202 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
2849164 55561 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1518183 55561 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1623233 55561 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
58062371 125353 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
CHEMBL3648384 125353 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
22254582 66638 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66638 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
2963624 36269 5 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
CHEMBL1447678 36269 5 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
44430455 86424 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86424 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430475 86642 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 86642 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
49801837 138481 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 138481 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597851 138531 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 138531 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 138631 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 138631 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89691439 137720 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137720 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53320117 56428 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56428 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
11654412 197240 22 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 197240 22 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70695918 73228 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73228 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
25017033 19090 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19090 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
45485018 196934 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578784 196934 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
70691723 73219 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73219 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756754 91697 21 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 91697 21 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
54583912 60272 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760085 60272 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
44442063 93959 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 93959 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24818378 29438 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
CHEMBL1386141 29438 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
1479652 51452 13 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51452 13 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
653550 36910 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
CHEMBL1452812 36910 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
646509 24603 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
CHEMBL1344766 24603 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
44414391 79787 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 79787 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414540 79916 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 79916 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
11994138 141115 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL385347 141115 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
54585863 60319 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60319 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89702226 138783 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138783 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11596311 56422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70691722 73218 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73218 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
9806086 64876 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 64876 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
16756403 150410 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150410 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
46188603 121250 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121250 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
44417977 81884 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217193 81884 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
3825639 29615 13 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
CHEMBL1387472 29615 13 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
44394864 125677 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 125677 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948210 38179 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
CHEMBL1463698 38179 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
2424660 40159 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
CHEMBL1482022 40159 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
70695851 73105 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73105 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45487653 197329 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197329 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11994137 82152 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL217844 82152 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
23027830 195616 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568664 195616 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
54579974 3189 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3189 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3189 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
127030071 138647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 138647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691652 73125 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73125 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442065 93875 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 93875 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
11628328 193866 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 193866 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
16755871 92063 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92063 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44417941 96142 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL263171 96142 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11511219 65804 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65804 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416828 141211 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385883 141211 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44416949 141261 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL386188 141261 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416272 79614 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212883 79614 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416212 80510 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215334 80510 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
54583953 60300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760224 60300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
9824428 65925 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 65925 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44416975 141298 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL386397 141298 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
44405560 72103 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72103 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
16192403 38340 2 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
CHEMBL1464847 38340 2 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
70685397 73217 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73217 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695917 73225 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73225 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46892401 125362 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
CHEMBL3648393 125362 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
90666257 108879 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 108879 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45485002 196844 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577913 196844 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11222404 193708 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 193708 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031356 138661 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 138661 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70685398 73229 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73229 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687550 73267 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73267 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756185 149189 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149189 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
20817761 76915 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 76915 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
90666252 108874 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 108874 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10434776 125861 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125861 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11653882 140774 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 140774 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
54581980 60268 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760081 60268 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
16756639 92798 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 92798 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
46850889 59243 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1717204 59243 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
54586826 60307 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760231 60307 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2310853 55920 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1335094 55920 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1626478 55920 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
11510887 81857 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 81857 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
52918017 60323 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60323 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44143496 191489 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 191489 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
56597542 138422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 138640 22 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 138640 22 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11502008 56278 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56278 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70689525 73159 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73159 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693808 73272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756073 91856 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 91856 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10324628 141693 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 141693 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 166809 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 166809 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
45487384 195166 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 195166 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
44438755 93070 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93070 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
44394591 122143 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122143 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
16756401 150409 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150409 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
46172921 59032 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
CHEMBL1706988 59032 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
2649486 29743 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
CHEMBL1388448 29743 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
11974227 168739 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 168739 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
2491454 46587 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
CHEMBL1540447 46587 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
127031621 138565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786572 138565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
16665072 98086 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98086 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
10047339 70062 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70062 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10250850 72066 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72066 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44403765 135337 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135337 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
49865976 16041 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16041 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11282448 62246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
16193698 32854 3 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
CHEMBL1416734 32854 3 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
11994662 140982 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL384553 140982 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
23120575 194200 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 194200 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44430452 149226 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149226 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
56598130 138620 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 138620 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
21939915 64385 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64385 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9983233 75648 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 75648 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348022 76998 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 76998 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
44394569 65885 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 65885 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405618 71671 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 71671 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
46172934 58920 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1702876 58920 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
46846323 59617 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1731906 59617 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
44438753 93027 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93027 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
58062362 125340 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
CHEMBL3648371 125340 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
70681115 73113 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73113 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
1431538 28989 4 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
CHEMBL1382150 28989 4 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
3229425 51368 2 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
CHEMBL1583768 51368 2 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
90666095 108840 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 108840 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
90666096 108841 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 108841 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10258364 193116 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
70693733 73128 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73128 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46933538 16040 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16040 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10360874 64603 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64603 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11994414 79906 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
CHEMBL214181 79906 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
11995342 80109 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL214808 80109 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
11995245 80175 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214991 80175 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
44416890 80079 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214705 80079 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44417044 80826 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215868 80826 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416377 80682 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215565 80682 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995444 80053 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214663 80053 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11994017 80591 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215364 80591 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
57522946 76033 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76033 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
11994019 141125 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
CHEMBL385391 141125 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
57522947 76034 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76034 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11995442 81865 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
CHEMBL217159 81865 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
11995345 141016 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
CHEMBL384770 141016 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
11995344 80186 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL215039 80186 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
18436119 76029 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76029 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44416875 79975 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214476 79975 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44414357 79343 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79343 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030367 138534 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 138534 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317305 56410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70693732 73115 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73115 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683287 73224 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73224 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394922 65810 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 65810 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394726 65828 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 65828 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394860 65916 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 65916 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10361342 122409 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122409 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10248906 123136 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123136 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
9828622 96206 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
CHEMBL263702 96206 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
45279489 123063 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123063 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
49865975 16039 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16039 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
135478067 23667 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
135485243 23667 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
154780186 23667 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
CHEMBL1336601 23667 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
70687471 73121 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73121 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45273887 121249 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
CHEMBL3589138 121249 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
11974030 154737 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 154737 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11995646 79870 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL213966 79870 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
54582957 60299 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760223 60299 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430453 87494 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87494 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
70681113 73109 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73109 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687549 73263 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73263 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70681215 73265 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73265 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693810 73278 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73278 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10075375 75649 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 75649 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11994275 82002 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
CHEMBL217356 82002 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
44417140 79844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL213864 79844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416851 141310 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
CHEMBL386460 141310 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
44416858 165551 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL425982 165551 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
54581466 60249 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760003 60249 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
24997711 58908 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
CHEMBL1702161 58908 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
46835796 58936 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
CHEMBL1703306 58936 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
46846326 59056 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708047 59056 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846335 59084 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1709509 59084 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172916 59326 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1720787 59326 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
44417986 165521 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425801 165521 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394573 123165 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123165 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
54579972 60317 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760244 60317 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
44417968 81164 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216241 81164 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416303 138138 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL377758 138138 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
4881730 51620 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
CHEMBL1585808 51620 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
54580923 60269 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760082 60269 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
70695855 73129 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73129 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11712898 178609 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 178609 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70687538 73227 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73227 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756641 142057 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142057 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
54585827 60270 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760083 60270 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
6463414 46922 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
CHEMBL1543278 46922 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
44414571 79865 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 79865 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
21062998 64384 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64384 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798744 138943 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138943 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
70691650 73111 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73111 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693737 73158 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73158 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57391573 68508 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922257 68508 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46846325 58889 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1701512 58889 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846316 59069 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708651 59069 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
24794275 23564 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
CHEMBL1335692 23564 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
16191953 52032 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
CHEMBL1589399 52032 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
90666259 108881 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 108881 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
56597407 138525 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 138525 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
123471111 138608 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 138608 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53318801 56407 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56407 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
21108114 67732 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 67732 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
70695930 73271 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73271 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
70693809 73276 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73276 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
10437982 92139 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92139 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
22348219 76171 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76171 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
21062991 64370 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64370 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70685395 73199 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73199 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44394644 65805 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 65805 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405487 71531 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71531 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46850891 58869 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
CHEMBL1700476 58869 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
10480652 64990 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 64990 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
10332650 65863 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 65863 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
44414392 79788 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 79788 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030368 138448 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138448 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
44442144 154157 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154157 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70691725 73230 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73230 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70683300 73262 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73262 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44414542 79925 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 79925 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54582015 60305 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760229 60305 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683237 73106 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73106 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70681117 73118 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73118 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
16756642 92847 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 92847 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44405464 165798 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 165798 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
46846321 59426 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1724571 59426 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
935062 46176 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1536967 46176 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
11995140 140946 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384371 140946 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
54582476 60267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
CHEMBL1760080 60267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
16756753 91696 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 91696 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
44394605 66683 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 66683 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11993897 96936 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL269695 96936 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
90666262 108885 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 108885 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
9844702 64376 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64376 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
49866036 16055 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16055 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
46850890 58807 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
CHEMBL1698073 58807 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
46172918 59101 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
CHEMBL1710128 59101 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
11995026 141375 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
CHEMBL386900 141375 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
44405408 72089 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72089 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44397221 66796 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 66796 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
54585376 60263 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760071 60263 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
70693620 72798 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011529 72798 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
69603769 73103 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73103 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70695859 73155 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73155 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
90666261 108884 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 108884 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70685408 73258 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73258 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
11974231 82008 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 82008 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
46835791 59044 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1707743 59044 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46172919 59543 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
CHEMBL1729021 59543 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
46172935 59650 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1733129 59650 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
11995137 141025 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384825 141025 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416362 165221 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL424723 165221 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485063 195692 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL569204 195692 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522945 76032 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76032 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
70691653 73134 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73134 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687477 73153 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73153 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11561126 68519 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68519 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44417949 81878 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217171 81878 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
18436114 74543 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74543 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
18435902 76022 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76022 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57523087 1136 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1136 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1136 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
23027211 195574 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 195574 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
21939937 64386 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64386 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11995552 79872 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL213973 79872 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995138 81864 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217158 81864 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
56597991 138646 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 138646 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
10159452 74495 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74495 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689594 73200 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73200 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394891 64884 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 64884 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
57400241 68507 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922256 68507 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
70687361 72799 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
CHEMBL2011532 72799 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
46835788 59586 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1730555 59586 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
70685346 73150 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73150 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44438745 93425 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93425 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414342 77682 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 77682 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54583954 60311 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60311 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394826 66272 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66272 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
11440762 81729 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 81729 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
11531660 135071 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135071 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
54585375 60262 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760070 60262 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
46835793 58994 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
CHEMBL1705499 58994 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
11973801 141436 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141436 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
90666254 108876 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 108876 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
70691724 73222 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73222 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11995346 81078 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL216008 81078 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11974228 79962 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 79962 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
71816518 137756 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137756 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442097 93576 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 93576 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44417862 80219 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80219 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
22348140 168158 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168158 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
11648240 71117 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71117 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
16739263 92981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 92981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
90666264 108887 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 108887 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127031339 138645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787457 138645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
1314 3670 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3670 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3670 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
23593468 64373 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64373 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70683299 73260 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73260 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44414310 137953 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 137953 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
54585864 60321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430478 86825 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 86825 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
127031623 138619 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787131 138619 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
45279402 123072 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123072 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
16756187 92741 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 92741 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
20817800 70074 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70074 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
57404374 72801 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011535 72801 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
44417988 82009 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217403 82009 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
71227161 128665 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 128665 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691651 73117 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73117 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691737 73269 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73269 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11684745 15915 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 15915 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417943 82066 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217678 82066 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
23658492 178399 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470633 178399 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
44405430 71605 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71605 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
10083869 65243 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
20817864 75707 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 75707 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
45484974 195613 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL568649 195613 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
44394883 125843 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 125843 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
54579971 60312 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760238 60312 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46835797 59439 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1725011 59439 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
11632909 132920 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 132920 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10377914 122658 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 122658 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
90666256 108878 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 108878 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
21062999 64287 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64287 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
46172937 58801 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
CHEMBL1697929 58801 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
11975436 78683 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 78683 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
3202885 40441 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
CHEMBL1484343 40441 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
11995139 82411 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL218031 82411 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562500 186153 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186153 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
44438747 92942 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 92942 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
54584857 60271 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760084 60271 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
46835810 58813 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1698337 58813 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
53318593 56416 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56416 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11605775 15865 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 15865 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405570 71648 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71648 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11994277 81228 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL216356 81228 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
15987265 195212 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 195212 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44425834 150884 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 150884 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417957 141373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL386880 141373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416777 80154 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214908 80154 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
44416872 80179 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215008 80179 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416838 80431 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL215256 80431 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417146 140901 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL384132 140901 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416955 140921 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL384233 140921 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416935 141132 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385410 141132 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417066 141420 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387217 141420 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416302 79638 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212958 79638 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416231 168424 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL439146 168424 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11201645 71527 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71527 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11995441 141429 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
CHEMBL387266 141429 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
57396294 67746 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67746 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 67742 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67742 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
1314 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
9865843 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
CHEMBL178707 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
11995243 82140 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217812 82140 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
11654412 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
11994661 82011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL217410 82011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
21940083 64387 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64387 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
127031355 138638 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787345 138638 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
23532180 68509 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922258 68509 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57403785 68520 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68520 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410876 75752 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 75752 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
45279868 123074 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123074 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
46172920 58942 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1703562 58942 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
45382322 59375 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
CHEMBL1722551 59375 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
11995645 141022 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384805 141022 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995647 141458 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL387420 141458 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562415 176391 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176391 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44394770 123322 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123322 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417971 141011 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL384734 141011 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11692293 93026 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93026 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417841 81178 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81178 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44405486 139982 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 139982 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405412 71530 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71530 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44405468 132911 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 132911 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
11974130 79952 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 79952 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394921 65908 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 65908 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
90666097 108842 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 108842 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666265 108888 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 108888 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430465 92867 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 92867 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
20817763 140053 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140053 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410904 171890 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171890 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394769 66581 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66581 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
54580458 60257 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760061 60257 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
22254581 65893 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 65893 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44396952 66395 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66395 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397262 67168 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67168 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44394705 124801 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 124801 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10262766 66645 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66645 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70685338 73133 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73133 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689595 73214 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73214 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11691995 15942 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 15942 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
44397425 66543 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66543 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
16756638 92797 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 92797 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
46172939 59531 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1728621 59531 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46835805 59536 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
CHEMBL1728794 59536 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
44438750 92980 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 92980 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414455 79862 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 79862 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
70685347 73162 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73162 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44410849 137769 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 137769 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44405651 71586 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71586 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
46172942 58833 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1698879 58833 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
70691739 73277 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73277 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405619 72159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44397127 66748 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 66748 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
49866087 16067 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16067 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
70693796 73221 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73221 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16755870 143953 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 143953 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756402 92414 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92414 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
46172928 59396 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1723453 59396 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172932 59567 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
CHEMBL1729749 59567 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
70693794 73211 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73211 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
44414499 79917 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 79917 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
23027181 195532 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568209 195532 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44562563 173788 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 173788 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11452268 81161 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81161 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
23532172 68510 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922259 68510 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
44394859 65914 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 65914 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46846324 59098 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1710048 59098 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846320 59667 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
CHEMBL1733974 59667 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
11974346 140968 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 140968 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11612098 69941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 69941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44395076 66661 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66661 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
44414518 77556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 79771 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 79771 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666266 108889 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 108889 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23120572 194389 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 194389 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
70683241 73156 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73156 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73164 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73164 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442064 154270 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154270 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
70683286 73208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11975438 79822 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 79822 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
23027527 195117 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 195117 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57393332 68518 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68518 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68519 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68519 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
70687552 73274 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73274 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11993895 79972 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214468 79972 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
11305934 3788 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
1315 3788 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
CHEMBL2147477 3788 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
11993896 80691 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL215591 80691 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
56589628 67807 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67807 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44416845 80133 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL214824 80133 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416814 80404 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL215234 80404 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
44416815 140942 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384346 140942 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
44417151 141023 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL384806 141023 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
44417145 141051 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL384988 141051 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416315 79424 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212137 79424 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416376 140895 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL384113 140895 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
23022536 76031 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76031 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
57523086 76038 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76038 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
23027402 195615 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568663 195615 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
22251624 64381 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64381 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57521366 76042 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76042 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44414570 77685 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 77685 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
11531010 133065 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133065 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
45485043 195529 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
CHEMBL568183 195529 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
49865738 15940 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 15940 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16755968 92060 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92060 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394650 65151 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65151 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
11974229 82071 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82071 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11778029 65877 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 65877 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
127031908 138642 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787417 138642 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11553648 73131 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73131 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
46850886 59603 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
CHEMBL1731173 59603 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
70691721 73209 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73209 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417828 80269 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80269 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44410823 75203 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75203 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
44410821 76770 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 76770 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16755872 92064 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92064 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44405459 132635 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 132635 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
44417931 141062 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
CHEMBL385037 141062 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
22254632 123577 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 123577 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
11995240 80688 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
CHEMBL215580 80688 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
70695914 73210 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73210 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11603897 123809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 123809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394763 66717 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 66717 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
46835800 59035 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1707135 59035 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46835816 59734 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1736481 59734 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
49865790 15966 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 15966 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485038 195607 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568604 195607 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
54584905 60310 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760236 60310 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44405612 134956 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 134956 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
1091600 27623 14 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
CHEMBL1371138 27623 14 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
49865929 16020 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16020 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
21062990 64369 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64369 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11591644 15914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 15914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16756186 92740 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 92740 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
10389978 69271 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69271 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
887424 55877 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1582334 55877 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1626085 55877 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
90666263 108886 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 108886 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
10025899 76712 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 76712 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11512135 69965 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69965 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11201867 98233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
70691656 73161 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73161 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562564 188549 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 188549 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
54585374 60258 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760062 60258 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
16756184 91707 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 91707 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
46172936 58953 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
CHEMBL1703918 58953 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
44394958 66571 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66571 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
20817762 76972 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 76972 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
46835813 59644 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1732922 59644 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46835807 59689 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
CHEMBL1734822 59689 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
11994018 80609 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215374 80609 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11995445 82034 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL217535 82034 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
9887864 178505 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
CHEMBL471651 178505 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
52917998 60308 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60308 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23022422 74542 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74542 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10274635 68517 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68517 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
10360874 64603 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64603 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
44394698 65909 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 65909 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
1305 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
57392824 67741 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67741 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11548234 70852 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70852 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45485028 195490 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567950 195490 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
18436066 74545 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74545 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11995443 79992 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214532 79992 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
16043291 79583 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79583 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
9910346 64401 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64401 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
44417022 79986 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214512 79986 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44417083 80498 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215298 80498 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
54580457 60255 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60255 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23120550 194931 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 194931 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
127033945 138424 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138424 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44394725 65820 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 65820 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44405482 71507 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71507 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
57395049 68501 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922250 68501 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46172917 59224 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
CHEMBL1716369 59224 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
11775505 141455 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141455 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
127031354 138575 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 138575 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44562600 172560 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 172560 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
49865679 15885 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 15885 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11419666 122038 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122038 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
16756752 142059 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142059 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
10137322 148876 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 148876 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44410838 76708 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 76708 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16756751 92878 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 92878 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
44397128 123583 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 123583 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
46172930 59718 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1735852 59718 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
11328029 76177 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76177 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
11634061 191755 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 191755 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
70693792 73201 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73201 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73203 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73203 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10388797 71415 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71415 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
46835804 59164 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1713871 59164 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
127033095 138541 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786352 138541 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
46835802 59107 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1710499 59107 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
49865869 16001 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 16001 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397026 126649 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 126649 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44417946 82040 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217557 82040 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
58062359 125354 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
CHEMBL3648385 125354 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
44438740 93503 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93503 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
46892785 125361 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
CHEMBL3648392 125361 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
44418005 81982 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217257 81982 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
11974345 79930 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 79930 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11259253 82133 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82133 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
90469437 120757 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120757 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44394798 123866 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 123866 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
11995136 80500 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL215307 80500 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
49865708 15913 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 15913 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485061 197076 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 197076 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44442090 93726 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 93726 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
10067783 65868 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 65868 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
44414451 168373 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168373 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
18436083 74540 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74540 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994136 141406 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
CHEMBL387085 141406 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
18436055 74525 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74525 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
90666260 108882 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 108882 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
11662906 73132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46172923 59073 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
CHEMBL1708907 59073 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
3114950 37536 29 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37536 29 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
44562403 189236 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189236 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
45485003 196697 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL576665 196697 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
11583835 73135 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73135 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666253 108875 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 108875 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
44394607 123834 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 123834 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11569300 82070 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82070 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
45382327 58938 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
CHEMBL1703414 58938 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
70687478 73154 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73154 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11619850 75424 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75424 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
23657037 94088 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94088 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693793 73207 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73207 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44592256 188786 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL512873 188786 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
11973916 140964 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 140964 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
54582014 60303 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760227 60303 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
46835792 59347 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
CHEMBL1721648 59347 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
2042108 47720 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
CHEMBL1549996 47720 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
58062337 125355 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
CHEMBL3648386 125355 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
45271839 194872 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 194872 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44442139 94022 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94022 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
49865680 15886 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 15886 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 15941 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 15941 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11649549 93504 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93504 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
70685396 73213 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73213 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11776033 66836 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 66836 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11995241 80149 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
CHEMBL214891 80149 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
1314 3670 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3670 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3670 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11190261 62913 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 62913 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
11592199 15943 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 15943 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
20817846 138167 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138167 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10456755 70754 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70754 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395019 65905 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65905 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
70681197 73215 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73215 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10344176 66849 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66849 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
4033 1868 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
9826520 1868 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
CHEMBL214957 1868 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
44397194 66647 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66647 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44394638 123282 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123282 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
52917999 60320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430458 142279 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142279 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
70696356 74493 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74493 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70685337 73126 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73126 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16068 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16068 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
11281523 81390 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81390 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
11153928 165227 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165227 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
23593464 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436075 74496 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74496 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57401509 67745 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67745 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
23593464 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11995028 140906 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
CHEMBL384147 140906 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
45485077 195527 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL568162 195527 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
11547939 160736 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
CHEMBL412135 160736 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
44414483 79323 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79323 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45267577 194294 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 194294 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11165058 154095 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154095 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
11633862 178588 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 178588 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10083869 65243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
10083869 65243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397476 67088 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67088 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
44417981 165428 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425269 165428 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
54582961 60316 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60316 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
21939767 64367 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64367 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70689519 73110 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73110 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689596 73216 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73216 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394596 65873 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 65873 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11554989 178485 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 178485 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
10070680 71765 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 71765 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
56597990 138655 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787582 138655 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
11526824 15944 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 15944 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405557 132230 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132230 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
1017287 55731 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1568072 55731 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1624689 55731 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
45268470 194621 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 194621 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
45268465 194886 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 194886 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
54585861 60304 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760228 60304 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2729502 80640 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 80640 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
46172925 59158 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
CHEMBL1713683 59158 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
44417972 141061 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385036 141061 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
90666267 108890 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 108890 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
49865927 16018 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16018 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
44417952 141210 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385876 141210 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973800 81160 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81160 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442071 154077 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154077 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
49865871 16003 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 16003 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49866086 16066 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16066 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11634230 69831 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69831 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
46835794 59226 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1716381 59226 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
1746683 31084 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
CHEMBL1401638 31084 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
11520239 3575 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
1313 3575 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
CHEMBL185271 3575 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
11236807 81154 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
16037921 139643 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380371 139643 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945130 16868 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254563 16868 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44412852 137875 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377321 137875 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943873 16853 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254400 16853 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52945087 16854 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254401 16854 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
11191034 79454 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212256 79454 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942885 16860 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254481 16860 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
10230947 72237 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199274 72237 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413473 96823 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL268938 96823 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413297 137884 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377372 137884 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44413474 166905 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL429895 166905 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52948758 16859 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254480 16859 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945129 16867 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254562 16867 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52950112 16894 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254797 16894 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417918 81135 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216103 81135 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
44417928 95970 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL261964 95970 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
23626228 88895 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL236889 88895 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417919 80461 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215278 80461 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
44417905 82060 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217637 82060 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52949912 16847 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254328 16847 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44424263 85360 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229406 85360 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
44434153 144709 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL391275 144709 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
44417993 81353 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216406 81353 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
10303281 133043 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL371099 133043 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44417922 82141 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL217820 82141 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
20609028 138366 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378269 138366 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11592317 138995 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL379521 138995 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44418004 168256 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL437728 168256 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
11236807 81154 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11236807 81154 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
52947407 16828 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254148 16828 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11634329 141768 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL388524 141768 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
11634329 141768 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
CHEMBL388524 141768 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
20608975 77410 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209089 77410 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434151 89184 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL237531 89184 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
10166088 72065 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
CHEMBL198724 72065 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
44413138 138365 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378261 138365 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52947140 16936 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255054 16936 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413326 79453 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212254 79453 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946021 16772 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253628 16772 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11236807 81154 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11156790 77579 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209510 77579 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
16659197 96635 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL267320 96635 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10311798 79579 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212750 79579 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
10128764 77905 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210857 77905 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417901 79905 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL214178 79905 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
44417895 165302 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL424895 165302 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44424260 85351 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229348 85351 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
44417967 81885 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217196 81885 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
10143980 72136 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198945 72136 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943978 16757 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253196 16757 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52947331 16800 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253875 16800 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52942540 16830 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254150 16830 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943913 16866 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254561 16866 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52949472 16883 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254714 16883 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945155 54691 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254636 54691 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615721 54691 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
44413475 77654 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL209754 77654 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
11497179 79358 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211820 79358 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417950 172185 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL450942 172185 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44413470 77988 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211069 77988 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417923 82169 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL217875 82169 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44405437 71604 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197280 71604 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405417 72209 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199179 72209 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405461 71512 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197005 71512 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
52941493 54693 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254564 54693 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615759 54693 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
10196608 76958 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208275 76958 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10312244 138983 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL379489 138983 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
11691468 168778 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL441886 168778 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
16659239 141351 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL386717 141351 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
15982955 93215 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL246794 93215 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10239929 77748 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210255 77748 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11692382 168808 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL442084 168808 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
44434148 89087 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237318 89087 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
52944859 16793 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253795 16793 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44434155 168829 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL442244 168829 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
44413428 78207 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
CHEMBL211232 78207 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
10196214 77777 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210344 77777 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405439 72143 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198969 72143 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129058 138136 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL377738 138136 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44417916 81725 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216741 81725 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10239448 77806 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210436 77806 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52944540 16884 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254715 16884 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44417913 81177 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216314 81177 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
10143421 72004 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198483 72004 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44434149 148122 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL393959 148122 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
20608974 79472 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212330 79472 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
17989329 80669 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL215508 80669 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
20608989 77831 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210532 77831 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44412960 79559 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL212671 79559 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
10174984 77755 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210274 77755 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945048 16845 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254326 16845 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948916 16848 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254329 16848 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
10209344 122738 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL361392 122738 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10165503 125432 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL364871 125432 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946184 16836 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254240 16836 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52942685 16858 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254479 16858 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946082 16801 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253876 16801 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52941054 16937 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255055 16937 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11317465 137673 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL376976 137673 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413472 138162 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377864 138162 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417926 80711 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215660 80711 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
52941272 16812 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253963 16812 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52947141 16939 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1255057 16939 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
23573799 72054 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198689 72054 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
10196316 77830 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210531 77830 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943353 16882 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254713 16882 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
70681299 73614 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
CHEMBL2021397 73614 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
10218547 77382 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208970 77382 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44434143 88894 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL236888 88894 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
11657090 79320 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL211615 79320 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417909 157171 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL408198 157171 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
11628547 138741 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL379060 138741 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417969 81165 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216242 81165 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44405435 72142 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198968 72142 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10218604 138337 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378180 138337 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417953 81173 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216280 81173 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52943912 16865 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254560 16865 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44417904 79967 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL214432 79967 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
10174522 139151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379797 139151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417900 81125 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216050 81125 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44417933 140978 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL384546 140978 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
20608996 77402 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209059 77402 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
20608991 77400 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209050 77400 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52946062 16794 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253796 16794 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412837 76922 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL208081 76922 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
11433168 138164 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138164 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413309 138379 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378310 138379 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949812 16818 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254055 16818 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10165656 71474 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196864 71474 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943485 16938 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255056 16938 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10129026 77901 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210818 77901 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405399 135474 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373165 135474 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943712 16820 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254057 16820 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44592215 188244 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
CHEMBL506480 188244 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
10196098 77669 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209828 77669 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10289494 77879 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210715 77879 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196460 79428 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212159 79428 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44592169 178254 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
CHEMBL469343 178254 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
44592214 188767 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL512657 188767 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
44417887 140952 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384400 140952 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52948636 16840 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254244 16840 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11570040 77416 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209109 77416 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11698592 77703 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209993 77703 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11613696 134732 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL372551 134732 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413283 79327 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211672 79327 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
20609018 139626 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380275 139626 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52948553 16802 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253877 16802 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945088 16856 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254403 16856 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
44417924 140874 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL384030 140874 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
44417892 79826 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL213771 79826 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
44405501 71535 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197065 71535 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
44413299 77017 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208573 77017 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413312 79237 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211511 79237 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949479 16896 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254799 16896 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44424266 85361 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229407 85361 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
11664086 77360 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208931 77360 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417889 140873 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384000 140873 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
10312086 79441 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212210 79441 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52946137 16817 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254054 16817 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52940981 16907 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254885 16907 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417960 81384 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL216429 81384 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
10186370 71465 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196819 71465 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
11642443 77274 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208827 77274 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
52947314 16791 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253793 16791 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
11318709 139139 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379789 139139 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434156 144995 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL391496 144995 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
10152879 78447 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211285 78447 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52945863 16922 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254972 16922 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947542 16861 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254482 16861 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947539 16852 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254399 16852 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11635274 138159 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377843 138159 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942539 16827 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254147 16827 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
20608977 138722 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378972 138722 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11628136 77422 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209123 77422 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
20608976 77776 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210343 77776 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434144 166755 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL429393 166755 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
11527169 77026 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL208635 77026 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
44434146 89012 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237099 89012 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
20608992 77945 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211005 77945 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44413471 79205 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211492 79205 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44412682 78044 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211166 78044 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944920 16819 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254056 16819 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413345 140962 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
CHEMBL384449 140962 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
44417927 80674 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215526 80674 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52943689 16810 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
CHEMBL1253961 16810 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
52944577 16908 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254886 16908 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405421 71657 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197429 71657 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405418 135261 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373036 135261 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44412686 78615 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211311 78615 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196742 161172 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL413578 161172 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417963 165458 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL425445 165458 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52942547 16839 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254243 16839 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
52943420 16923 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254973 16923 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52948635 16837 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254241 16837 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946259 16846 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254327 16846 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44412624 77982 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211058 77982 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10129036 79414 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212093 79414 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11562056 79381 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211956 79381 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417893 80171 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL214983 80171 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
10152726 138200 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
CHEMBL378009 138200 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
44417912 81863 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217140 81863 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
11433168 138164 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138164 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947267 16773 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253629 16773 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948531 16792 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253794 16792 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44424270 85370 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL229463 85370 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
52943690 16811 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253962 16811 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
24963343 72802 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 72802 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
10239505 77577 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209504 77577 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44434154 89490 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL237959 89490 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
11512221 89393 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237748 89393 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
52947610 16873 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254634 16873 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10280331 140785 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL383390 140785 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
20608969 77818 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210481 77818 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44417920 80442 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215266 80442 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417987 82000 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217351 82000 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
20609011 138186 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377976 138186 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413480 79531 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL212573 79531 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
11635715 77090 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208688 77090 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
10239639 77799 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210408 77799 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52947054 16909 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254887 16909 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10281308 72021 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198562 72021 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413382 77414 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209103 77414 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11270012 81736 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216821 81736 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
52949955 16851 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254398 16851 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945806 16895 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254798 16895 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405436 71603 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197279 71603 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
11656916 138363 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL378242 138363 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417954 96811 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL268848 96811 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
44434152 89185 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237532 89185 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417898 82163 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL217860 82163 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
44405444 134675 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372116 134675 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129135 77692 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209935 77692 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
16106513 178304 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL469789 178304 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10218194 78010 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211139 78010 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413271 137865 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377270 137865 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
16659061 82164 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217861 82164 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
10239930 79229 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211504 79229 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52949693 16774 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253630 16774 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
20608981 79455 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212265 79455 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947408 16829 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254149 16829 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52941518 16874 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254635 16874 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943587 16775 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253631 16775 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10188732 134876 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372803 134876 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
44417934 82053 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217605 82053 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52949956 16855 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254402 16855 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
11497180 165212 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL424697 165212 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417929 81526 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216486 81526 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44417985 81152 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216187 81152 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
11752339 69056 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL193260 69056 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
10196576 138727 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL378994 138727 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52948951 16838 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254242 16838 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
52949768 16803 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253878 16803 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412683 78760 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211335 78760 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944948 16826 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254146 16826 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
44417891 79942 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214323 79942 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417908 81751 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216959 81751 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44413259 139160 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
CHEMBL379802 139160 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
44434145 89010 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237098 89010 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
10152629 141001 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL384676 141001 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413398 77593 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209590 77593 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11520239 3575 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3575 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3575 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
54579974 3189 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7756 3189 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
CHEMBL1760248 3189 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7735 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
9927967 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
CHEMBL400679 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
1305 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
9934033 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
CHEMBL182150 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1314 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
9865843 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
CHEMBL178707 3670 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
24890862 1088 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
7755 1088 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
57523087 1136 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
7754 1136 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
CHEMBL2059513 1136 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
57521365 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
57521365 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
8587 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
8587 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
CHEMBL2059420 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
CHEMBL2059420 2577 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
56835134 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
7753 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
CHEMBL1934835 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
4033 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
9826520 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
CHEMBL214957 1868 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
1292 1042 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1290 256 0 None 15 2 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1307 524 0 None -1 2 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
11305934 3788 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1315 3788 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
CHEMBL2147477 3788 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1300 3039 0 None - 1 Human 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
11539096 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1303 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
CHEMBL214021 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1297 3054 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1297 3054 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159839
1297 3054 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
11994411 989 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
1306 989 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
CHEMBL214523 989 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44219756 178115 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
CHEMBL468099 178115 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
44219756 178115 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
CHEMBL468099 178115 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
44442095 93866 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 93866 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11648912 79941 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 79941 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
45487671 195603 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568571 195603 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44574008 188636 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL511542 188636 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
9915039 60498 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL176219 60498 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
45487668 195322 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566880 195322 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
45271549 193900 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 193900 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
24762415 197070 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL582978 197070 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44417966 160971 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 160971 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 168453 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 168453 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10118862 60478 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL176159 60478 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
45487674 197047 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL582792 197047 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
10258364 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538424 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538425 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
18436066 74545 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74545 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10258364 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10360874 64603 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64603 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10230490 62849 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL178997 62849 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
10345845 177898 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 177898 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
22018957 82030 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82030 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11561126 68519 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68519 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68519 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL1922270 68519 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
18436114 74543 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74543 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
9932896 74178 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74178 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
9932896 74178 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74178 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10004545 74603 4 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
46933538 16040 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16040 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417832 141220 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141220 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10258364 193116 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10459635 195020 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL564788 195020 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
18436055 74525 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74525 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
70696356 74493 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74493 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417948 141217 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141217 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22348140 168158 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168158 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
45273335 194157 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL558305 194157 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
10114686 60246 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175993 60246 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
10067783 65868 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 65868 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10000146 64316 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64316 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11201645 71527 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71527 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57393332 68518 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68518 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410849 137769 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 137769 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
90666096 108841 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 108841 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44407944 165449 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165449 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70688018 74494 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74494 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11705240 132292 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132292 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
18436094 74536 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74536 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
21108114 67732 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 67732 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10226765 122620 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL361215 122620 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394650 65151 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65151 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394800 121842 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 121842 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394609 123367 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123367 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
10248906 123136 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123136 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
16721015 80011 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80011 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11583193 141277 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL386281 141277 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018944 81796 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 81796 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
22018964 141138 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141138 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
56835134 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
7753 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
CHEMBL1934835 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
25058425 60449 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761103 60449 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114286 60465 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761119 60465 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
57890345 121890 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
CHEMBL3600810 121890 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
60130264 121891 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
CHEMBL3600811 121891 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
10413283 186885 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL494016 186885 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
18436117 74544 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74544 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
44557554 194737 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 194737 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
9932896 74178 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74178 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10481477 194012 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL556697 194012 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
44417875 80382 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80382 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22348022 76998 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 76998 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
57521365 2577 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2577 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2577 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
10231341 63016 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL179437 63016 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
10113523 129294 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL367532 129294 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394769 66581 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66581 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10150552 81181 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81181 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417959 81383 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81383 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141285 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141285 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
57392823 67739 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 67739 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
22348155 76232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44555375 195127 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL565614 195127 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436038 76021 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76021 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417845 141354 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141354 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11627530 75557 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75557 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487660 197348 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL585856 197348 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10345845 177898 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 177898 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
18436085 74539 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74539 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522703 76023 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76023 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417846 81687 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 81687 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939937 64386 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64386 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11775399 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
CHEMBL179501 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
45487647 195246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566257 195246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436083 74540 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74540 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436082 74541 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74541 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11775399 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
CHEMBL179501 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
11713027 80762 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 80762 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
11775399 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63030 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11775399 63030 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL179501 63030 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44417998 81983 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 81983 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150954 141015 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141015 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11548234 70852 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70852 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10027853 71518 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71518 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57523087 1136 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1136 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1136 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
57523086 76038 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76038 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
11496313 71968 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71968 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21939898 64395 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64395 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
18435902 76022 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76022 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11613073 75577 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75577 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44573931 186869 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL493962 186869 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
23022536 76031 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76031 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
9932896 74178 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74178 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
22251624 64381 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64381 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23022422 74542 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74542 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
18435902 76022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10183297 92880 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
CHEMBL245231 92880 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
44402563 71328 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196388 71328 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
10005009 165823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21940083 64387 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64387 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10345121 186870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
CHEMBL493967 186870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
9910346 64401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522468 76041 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76041 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
57521365 2577 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2577 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2577 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
71730392 130770 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686821 130770 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730393 130771 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686822 130771 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730531 130778 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686829 130778 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44394763 66717 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 66717 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
44394683 66872 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 66872 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394591 122143 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122143 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123114 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123114 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394866 123830 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 123830 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11647458 81586 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216524 81586 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417925 81052 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81052 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141028 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141028 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
25115854 60447 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761101 60447 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70691736 73254 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73254 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57845728 121924 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600971 121924 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
122184694 121974 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601035 121974 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184706 121987 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601047 121987 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89798657 122019 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601303 122019 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
59835853 121847 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600392 121847 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
60130301 121893 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600813 121893 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
59835871 121957 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601014 121957 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
9866552 80090 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
CHEMBL2147476 80090 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
11646818 165671 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL426666 165671 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817846 138167 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138167 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44407967 74143 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74143 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271134 193456 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550068 193456 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
11166395 93840 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250327 93840 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666095 108840 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 108840 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70693734 73130 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73130 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865927 16018 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16018 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
16072132 80017 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80017 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
10344176 66849 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL187756 66849 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44397202 66888 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 66888 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44390730 63986 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181099 63986 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403548 70049 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70049 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403523 70076 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70076 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403498 70734 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 70734 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403506 70790 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 70790 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
10025637 65253 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL183215 65253 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
44413474 166905 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL429895 166905 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
12020151 193518 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550545 193518 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44405431 71607 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71607 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
44394644 65805 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 65805 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 130930 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 130930 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11562129 70733 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70733 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
60169181 87335 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337728 87335 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
54582961 60316 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60316 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
89691143 138785 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 138785 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
21108099 67815 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914860 67815 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18436118 74532 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
CHEMBL2031723 74532 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
23022589 74538 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031729 74538 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11633862 178588 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 178588 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10050565 75353 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75353 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403527 126654 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 126654 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403538 135588 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 135588 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44418001 141172 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385639 141172 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417822 80161 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214936 80161 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71717085 87354 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337747 87354 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71717701 87368 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337761 87368 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25115619 60443 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761097 60443 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
21939900 64368 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818780 64368 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
90666251 108873 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 108873 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70693737 73158 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73158 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
45269335 194789 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 194789 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44562522 192949 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL529450 192949 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71716478 87355 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337748 87355 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397303 66507 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186160 66507 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
155528494 170783 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
CHEMBL4461504 170783 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
11776033 66836 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 66836 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70693810 73278 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73278 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44407966 75542 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204912 75542 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
11605260 70292 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70292 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
44402535 165509 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL425744 165509 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
44442058 93921 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250728 93921 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49866089 16069 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16069 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44403499 70773 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 70773 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
70693792 73201 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73201 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10399674 65789 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184001 65789 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11569340 71306 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71306 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11677806 185427 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL487040 185427 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70685396 73213 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73213 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
71226697 128658 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128658 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730920 130705 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686755 130705 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759545 130722 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686772 130722 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730390 130767 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686818 130767 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759570 130769 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686820 130769 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417897 140893 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL384111 140893 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
70689612 73257 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73257 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
71816518 137756 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137756 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
21062999 64287 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64287 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
122184562 121896 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600816 121896 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978378 121953 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601010 121953 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89702226 138783 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138783 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57391028 67743 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67743 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57401510 67748 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 67748 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
56589628 67807 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67807 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11328029 76177 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76177 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
45271908 193861 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL554287 193861 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
23120582 194612 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562074 194612 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
45273802 193165 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
CHEMBL539475 193165 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
45487385 195167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
CHEMBL565834 195167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
45487356 196155 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572300 196155 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666094 108839 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 108839 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666262 108885 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 108885 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
11605775 15865 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 15865 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
127031338 138542 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 138542 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
49801837 138481 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 138481 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
123471111 138608 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 138608 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 138640 22 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 138640 22 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11563017 80650 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80650 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44405481 71506 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71506 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
89690237 137696 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 137696 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
54580457 60255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
117816753 138807 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 138807 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
89691057 138941 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 138941 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436095 74537 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031728 74537 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11592199 15943 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 15943 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865868 16000 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 16000 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397009 66426 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL185843 66426 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44397310 66975 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188401 66975 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403471 140812 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
CHEMBL383567 140812 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
23567394 60549 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176230 60549 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
10420382 165752 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL427153 165752 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417866 80137 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214843 80137 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417827 80690 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215586 80690 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417996 165550 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL425979 165550 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135474 91097 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403867 91097 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16192241 48472 4 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
CHEMBL1558309 48472 4 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
44394966 122446 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL360811 122446 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
11605260 70292 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70292 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
45272006 193568 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550943 193568 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44562501 185416 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
CHEMBL487022 185416 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
70695930 73271 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73271 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45268637 194503 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL561344 194503 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
49865929 16020 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16020 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562562 173786 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455143 173786 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11518159 134738 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372570 134738 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
3410248 70753 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL195350 70753 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
11973916 140964 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 140964 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
22254632 123577 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 123577 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
91759549 130731 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686781 130731 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683286 73208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
70689520 73119 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73119 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683241 73156 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73156 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
46899582 16771 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253627 16771 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45267849 194458 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL561092 194458 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44442059 93922 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250729 93922 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759566 130761 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686812 130761 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730391 130768 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686819 130768 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417921 80713 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 80713 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
10310161 96634 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL267319 96634 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018896 141162 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141162 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57392549 69301 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934837 69301 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89689924 137804 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 137804 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
52917999 60320 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60320 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
59835799 121962 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601019 121962 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
23593474 64372 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64372 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21062998 64384 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64384 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
21939915 64385 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64385 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
21940008 64394 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64394 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57399741 67747 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 67747 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11419337 165608 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL426292 165608 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
44410876 75752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 75752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410944 76699 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 76699 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10025899 76712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 76712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11973800 81160 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81160 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44143492 192853 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526647 192853 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522948 76035 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76035 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
53322554 56412 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642473 56412 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53320117 56428 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56428 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
90666266 108889 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 108889 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23022509 76028 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76028 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
18436119 76029 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76029 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57521366 76042 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76042 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407629 168089 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168089 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487653 197329 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197329 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11419337 165608 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL426292 165608 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10041636 122679 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 122679 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417838 81185 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81185 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
60168913 87348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337741 87348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57397816 69275 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934811 69275 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690573 137784 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 137784 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89690573 137784 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 137784 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89691019 138863 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 138863 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267724 194454 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL561083 194454 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
11561155 190314 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518515 190314 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
46902024 16920 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254968 16920 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44397560 67388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
CHEMBL190775 67388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
57396293 67735 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914626 67735 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390748 64021 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181251 64021 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417994 81354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL216407 81354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
70691721 73209 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73209 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44403501 69307 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69307 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44393379 64967 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL182886 64967 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
45270302 193749 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL552224 193749 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
44573964 178078 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
CHEMBL467668 178078 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
44407951 75024 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203804 75024 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
44562523 186179 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488887 186179 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44417902 80660 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL215457 80660 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
155527803 170704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4460423 170704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
71226697 128658 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128658 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730130 130749 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686800 130749 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730132 130751 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686802 130751 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730395 130775 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686826 130775 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730529 130776 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686827 130776 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730530 130777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686828 130777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417894 80172 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80172 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417973 140943 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 140943 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417823 165219 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165219 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417956 96203 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96203 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71117 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71117 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184701 121982 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601042 121982 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
122184702 121983 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601043 121983 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
52917998 60308 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60308 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89798658 122011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601295 122011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
56680348 64390 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64390 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89691096 138947 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138947 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11973799 82050 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82050 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
44407860 75070 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75070 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271095 193559 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL550876 193559 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
23022499 74497 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
CHEMBL2031577 74497 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
44442120 93815 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250123 93815 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11505089 193139 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 193139 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866035 16054 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16054 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522950 76037 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76037 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
24952418 91086 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91086 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
56598130 138620 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 138620 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407875 74712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 74712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44413326 79453 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL212254 79453 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
44394946 64944 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL182847 64944 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
44417867 140981 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 140981 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71718318 87362 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337755 87362 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
89690622 137808 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 137808 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798780 138861 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 138861 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798680 138847 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 138847 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798688 138938 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 138938 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
45268527 194788 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL563147 194788 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
155569743 85632 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL2308118 85632 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
23593471 64375 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818787 64375 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44394861 65881 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184454 65881 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44413138 138365 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL378261 138365 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10377914 122658 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 122658 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11974126 141421 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL387219 141421 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
91759553 130734 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686784 130734 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
11386451 71528 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197054 71528 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
44143500 192350 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL522242 192350 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
57402226 69061 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1933085 69061 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
10332650 65863 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 65863 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254571 66635 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66635 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
45270297 193683 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551826 193683 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
90666255 108877 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 108877 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
44442098 93614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248881 93614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
86695567 130709 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686759 130709 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
86695568 130710 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686760 130710 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759567 130764 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686815 130764 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
57392546 69280 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934816 69280 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397817 69281 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934817 69281 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
52918016 60322 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60322 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
1314 3670 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3670 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3670 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
56666754 64383 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64383 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89702566 138798 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 138798 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44407870 75561 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75561 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
90666265 108888 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 108888 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127030368 138448 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138448 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
56597851 138531 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 138531 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 79931 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79931 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
16659197 96635 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL267320 96635 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
44395019 65905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44395076 66661 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66661 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
89691440 137639 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 137639 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21062991 64370 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64370 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56673714 64389 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64389 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
117798675 138830 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 138830 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89690973 138834 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 138834 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691284 138892 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 138892 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273638 194069 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557317 194069 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
49865789 15964 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223967 15964 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11678370 136042 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136042 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11284878 64012 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181217 64012 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401626 71010 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195810 71010 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
44403539 165727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427006 165727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
45271246 193537 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550683 193537 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
57397818 69295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934830 69295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
70681114 73112 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73112 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45271647 193512 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550513 193512 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45273406 194727 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562788 194727 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
9804849 67117 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67117 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70687550 73267 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73267 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45271549 193900 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 193900 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
49866034 16053 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224304 16053 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11190261 62913 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 62913 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
44394983 65948 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 65948 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11974129 80702 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
CHEMBL215631 80702 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
44394825 65836 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184277 65836 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
60150483 73205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10408758 121906 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600826 121906 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
71226268 128662 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
CHEMBL3670641 128662 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
71225855 128664 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
CHEMBL3670643 128664 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
91759571 130772 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686823 130772 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
10025637 65253 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65253 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
57399486 69282 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934818 69282 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
122184698 121978 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601039 121978 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
122184704 121985 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601045 121985 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89702233 137674 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 137674 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184565 121899 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600819 121899 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44438748 148965 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 148965 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
22348066 165277 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165277 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
10024175 187454 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497619 187454 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
7735 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
9927967 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
CHEMBL400679 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
11419776 93816 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250124 93816 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666264 108887 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 108887 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70691652 73125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685338 73133 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73133 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865928 16019 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16019 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
71227161 128665 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 128665 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597988 138623 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 138623 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 79931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
44408027 74717 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 74717 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
44390710 64258 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181632 64258 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
71227171 128672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
CHEMBL3670650 128672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
44417967 81885 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
CHEMBL217196 81885 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
44417895 165302 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL424895 165302 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
10434776 125861 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125861 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405430 71605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
70691722 73218 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73218 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89690292 137660 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 137660 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025096 137699 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 137699 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
89691440 137639 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 137639 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127029759 138835 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
CHEMBL3793053 138835 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
53325163 56408 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642469 56408 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45270803 193409 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL549636 193409 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
90666257 108879 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 108879 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70695853 73122 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73122 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553648 73131 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73131 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685347 73162 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73162 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11526824 15944 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 15944 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562461 188313 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL507549 188313 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
44390499 129135 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367355 129135 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11284878 70098 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194602 70098 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
11656044 140606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 140606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184673 121934 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600981 121934 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
45267746 194762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL563005 194762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
44438739 93502 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248295 93502 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
16742745 121970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601031 121970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
44397716 167751 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL434156 167751 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
11662564 133003 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 133003 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395012 65962 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184797 65962 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11974345 79930 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 79930 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
22266820 203336 21 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL77072 203336 21 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
71226964 128659 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 128659 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71730663 122033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601376 122033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759548 130730 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686780 130730 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732079 130748 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686799 130748 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759579 130787 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686837 130787 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
9804849 67117 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67117 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 69979 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 69979 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44403742 71375 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL196573 71375 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
10388797 71415 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71415 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25114068 60462 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761116 60462 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685407 73253 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73253 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
9980157 121925 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600972 121925 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730663 122033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601376 122033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
89691096 138947 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138947 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11653882 140774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL383359 140774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817763 140053 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140053 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
9804849 67117 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67117 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
53318595 56430 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642493 56430 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44442134 93758 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249716 93758 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
56597542 138422 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138422 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627530 75557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407836 74916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11562138 70174 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70174 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
60168915 87349 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337742 87349 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690973 138834 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 138834 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45270157 193399 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL549583 193399 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
9895868 12790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL1188966 12790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL537846 12790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10231050 64003 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181184 64003 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9895868 69239 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69239 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403492 70285 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
CHEMBL195006 70285 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
44403490 71312 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196362 71312 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
18436043 76025 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059412 76025 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44397605 67169 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189508 67169 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44408093 140367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382126 140367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
49865870 16002 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224081 16002 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44394854 66580 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186547 66580 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11189610 165224 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165224 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44438741 93391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417937 141026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL384844 141026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
44388409 165686 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 165686 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
46902025 16935 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1255050 16935 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
70681198 73226 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73226 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562524 186180 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
CHEMBL488890 186180 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
11973802 81715 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL216680 81715 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
71731806 122012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3601296 122012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732078 122016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601300 122016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71731045 130753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686804 130753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730788 130801 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686851 130801 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
44417886 141166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
122184670 121926 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600973 121926 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
89702233 137674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 137674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71731806 122012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601296 122012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
71732078 122016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601300 122016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
21062990 64369 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64369 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
9844702 64376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
59835874 121964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601020 121964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89691044 138949 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 138949 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89690957 138795 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 138795 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57399741 67747 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 67747 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11692293 93026 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93026 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
23120580 194367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL560334 194367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407667 74057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
45267735 194643 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL562285 194643 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
45271673 193704 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL551924 193704 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
44250210 194273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
CHEMBL559535 194273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
70685337 73126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57401248 69277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934813 69277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
89702355 137672 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 137672 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798692 138816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 138816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
18436109 76026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059413 76026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417017 79970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 79970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11620005 81044 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81044 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397309 67188 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189602 67188 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44390707 129146 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367359 129146 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11973802 81715 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
CHEMBL216680 81715 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
44417825 141118 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385361 141118 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
70681197 73215 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73215 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417991 82021 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217459 82021 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
90666252 108874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 108874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45271663 194896 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL563884 194896 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
155516078 169483 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4442916 169483 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
10262766 66645 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66645 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11568782 71555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
46899578 16799 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253872 16799 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11974030 154737 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 154737 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11211551 166710 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL429301 166710 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
57399487 69294 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934829 69294 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
71226697 128658 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128658 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71225842 128663 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
CHEMBL3670642 128663 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
71730131 130750 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686801 130750 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730264 130760 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686811 130760 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730265 130762 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686813 130762 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759569 130766 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686817 130766 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
71730534 130789 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686839 130789 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759586 130798 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686848 130798 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730789 130802 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686852 130802 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71714121 122034 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122034 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
10173787 82026 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82026 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141236 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141236 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
89691044 138949 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 138949 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436126 74529 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031720 74529 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
53318592 56409 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
CHEMBL1642470 56409 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
53326457 56427 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642490 56427 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
10050565 75353 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75353 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139029 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139029 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408108 139284 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139284 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417979 81734 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 81734 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417940 81282 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81282 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11539632 70217 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70217 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
71718910 87343 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337736 87343 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89702355 137672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 137672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53324269 56426 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642489 56426 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687471 73121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11691995 15942 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 15942 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
45270416 194978 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL564409 194978 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44403733 72099 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
CHEMBL198823 72099 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
70693795 73212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45178545 172646 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
CHEMBL4522986 172646 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
44394987 65897 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184534 65897 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
90666259 108881 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 108881 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
44402420 140840 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL383798 140840 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
122184703 121984 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601044 121984 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
137655884 158212 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158212 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
11974035 82211 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
CHEMBL217925 82211 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
137655884 158212 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158212 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
71226964 128659 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 128659 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71225843 128660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670639 128660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
71731803 130704 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686754 130704 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730919 130718 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686768 130718 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730266 130763 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686814 130763 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759568 130765 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
CHEMBL3686816 130765 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
71731048 130795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686845 130795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730662 130796 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686846 130796 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL4115910 211204 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL None None None None nan
44417939 81970 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL217233 81970 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
9804849 67117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114723 60469 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761124 60469 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
89690396 137724 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 137724 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
23593468 64373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89702226 138783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57401507 67736 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914627 67736 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57392835 67809 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914854 67809 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44143493 187463 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497647 187463 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45273801 194032 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL556927 194032 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44573823 192631 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL523697 192631 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
70687477 73153 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73153 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522949 76036 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76036 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
9804849 67117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11612098 69941 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 69941 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11518384 165354 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL425013 165354 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
44417858 79971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214450 79971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71719523 87341 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337734 87341 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
21940052 64380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
17848895 67699 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914463 67699 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44403535 71083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196004 71083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44395007 123556 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL363264 123556 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
44401591 68555 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL192266 68555 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10377822 126303 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126303 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11837128 71786 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 71786 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
60168916 87350 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337743 87350 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44407836 74916 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74916 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394999 66327 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL185348 66327 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11440885 82059 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217626 82059 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
44403533 71112 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71112 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44397329 66782 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187447 66782 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
45267709 194297 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
CHEMBL559691 194297 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
44394958 66571 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66571 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403486 71166 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL196273 71166 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
11453830 63076 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
CHEMBL179606 63076 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
10466406 66016 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185095 66016 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44394891 64884 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 64884 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394726 65828 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 65828 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
22018856 80195 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80195 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
22018999 80707 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 80707 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417947 140979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 140979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22018945 141191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417845 141354 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141354 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25115618 60444 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761098 60444 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
9866745 121880 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600801 121880 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11743571 121882 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600803 121882 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184557 121883 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600804 121883 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
60130278 121886 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600807 121886 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11592099 93069 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93069 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
11562138 70174 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
CHEMBL194697 70174 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
10070016 71119 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL196208 71119 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
9983233 75648 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 75648 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11683903 82017 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82017 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
11201867 98233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
11583049 141416 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141416 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
23120572 194389 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 194389 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407629 168089 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168089 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436038 76021 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76021 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
57522947 76034 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76034 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11556070 193818 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
CHEMBL553196 193818 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
11628328 193866 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 193866 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
46933537 15887 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 15887 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522703 76023 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76023 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11583747 81083 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81083 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
11677277 141247 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141247 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
11598355 141271 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141271 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44390726 121889 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL360081 121889 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
11562138 70174 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70174 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
10047339 70062 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70062 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417962 81674 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 81674 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71588 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71588 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44573822 186882 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL494009 186882 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
44573821 192131 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL522037 192131 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
10224210 62981 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL179353 62981 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
11353174 80185 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215030 80185 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
44394798 123866 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 123866 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
21939950 64396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939937 64386 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64386 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
45267576 194957 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 194957 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18436115 74524 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031715 74524 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
44417843 81549 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81549 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11511219 65804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 69979 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 69979 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11655872 71373 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71373 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
11511219 65804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139029 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139029 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939898 64395 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64395 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44408109 75192 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75192 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522946 76033 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76033 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57523087 1136 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1136 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1136 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
44402677 71389 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196599 71389 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
21940083 64387 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64387 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
23120550 194931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 194931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
57522816 76030 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76030 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
10273126 60818 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176548 60818 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
45487640 195568 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568361 195568 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44469273 195881 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 195881 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
44394770 123322 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123322 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11583744 71380 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71380 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
22251624 64381 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64381 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
9887476 192820 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526083 192820 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
10391177 188665 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
CHEMBL511747 188665 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
10159452 74495 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74495 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57523086 76038 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76038 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
10391177 188665 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL511747 188665 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
10310316 80708 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 80708 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939902 64388 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64388 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
18436075 74496 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74496 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417877 80725 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 80725 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10073934 186907 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
CHEMBL494155 186907 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
71226400 128661 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670640 128661 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
44413472 138162 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377864 138162 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
71731671 130703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686753 130703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730917 130715 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3686765 130715 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
71730134 130754 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686805 130754 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730787 130800 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686850 130800 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730792 130807 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686857 130807 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44394922 65810 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 65810 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394959 66874 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66874 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44417905 82060 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82060 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44405618 71671 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 71671 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
44405560 72103 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72103 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405646 96425 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96425 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405557 132230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405612 134956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 134956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
11653882 140774 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 140774 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
10083869 65243 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65243 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10083869 65243 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417888 79995 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 79995 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417857 141124 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141124 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11632484 69991 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 69991 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
60169095 87331 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337724 87331 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396018 69278 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934814 69278 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394271 69279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934815 69279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394272 69285 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934820 69285 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401249 69286 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934821 69286 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57402992 69287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934822 69287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691725 73230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184692 121971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601032 121971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
16742747 121973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601034 121973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89691439 137720 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137720 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
10386162 121907 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600827 121907 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388352 121959 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601016 121959 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
21062999 64287 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64287 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
57398087 67733 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914624 67733 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
21108117 67813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914858 67813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
44438740 93503 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93503 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44442153 93613 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 93613 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44562545 188514 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 188514 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11583835 73135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522948 76035 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76035 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
44455414 96968 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
CHEMBL269939 96968 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
44397194 66647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44407710 73592 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73592 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
58646147 78675 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 78675 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403493 69449 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69449 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403454 71399 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71399 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403522 123540 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 123540 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 124671 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 124671 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126253 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126253 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403474 126705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 126705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403505 133047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403445 165824 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 165824 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403468 167866 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 167866 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403493 69449 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69449 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403523 70076 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70076 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403528 70201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403513 133756 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 133756 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44394799 65922 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 65922 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
44394948 65913 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184585 65913 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405459 132635 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 132635 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
9895868 69239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403477 71484 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71484 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44424072 85197 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85197 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
71719524 87357 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
CHEMBL2337750 87357 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
10421933 124125 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL364104 124125 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695914 73210 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73210 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417936 81180 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216323 81180 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
71720121 87363 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
CHEMBL2337756 87363 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
44403473 70136 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
CHEMBL194630 70136 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
70689595 73214 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73214 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73203 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73203 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70695859 73155 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73155 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
11272081 81046 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215964 81046 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71732074 130724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686774 130724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730664 130799 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686849 130799 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759587 130804 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686854 130804 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
44417899 141041 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
CHEMBL384919 141041 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
11563383 70171 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70171 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
70681216 73266 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73266 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184672 121932 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600979 121932 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
54585863 60319 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60319 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23593468 64373 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64373 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89690864 138909 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 138909 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267714 194362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL560283 194362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
45267430 193145 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
CHEMBL538993 193145 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
49865654 15867 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 15867 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
24952055 91089 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91089 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10070680 71765 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 71765 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394604 124530 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 124530 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394807 65886 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 65886 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44417975 141328 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141328 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
71718317 87359 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337752 87359 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
127025096 137699 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 137699 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
23593472 64374 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64374 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
117798688 138938 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 138938 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89691193 138880 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 138880 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44408081 74707 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203549 74707 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407934 75578 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205112 75578 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
25114724 60471 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761126 60471 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
70695854 73123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73164 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73164 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442062 93958 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250926 93958 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44562480 185324 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL486878 185324 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
70681115 73113 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73113 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
89790062 130714 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686764 130714 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730918 130716 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686766 130716 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44417873 81047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
6621104 66468 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL185997 66468 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
11634230 69831 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69831 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184705 121986 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601046 121986 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
44193625 122032 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601375 122032 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
71714121 122034 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122034 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
9844702 64376 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64376 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11510887 81857 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 81857 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442118 93874 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250530 93874 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11577588 194166 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL558442 194166 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666267 108890 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 108890 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11662906 73132 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73132 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11684745 15915 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 15915 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44408028 140373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70691333 77618 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77618 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
44405487 71531 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71531 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691723 73219 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73219 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
21062991 64370 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64370 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
69603769 73103 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73103 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44403491 71423 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196686 71423 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403516 69951 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 69951 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
11204090 69493 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193771 69493 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403750 133390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
CHEMBL371576 133390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
70691737 73269 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73269 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70689519 73110 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73110 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562521 186178 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488886 186178 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
155562407 174635 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4571110 174635 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
71226938 128667 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
CHEMBL3670646 128667 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
71226243 128674 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
CHEMBL3670652 128674 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
71731050 130757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686808 130757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
10389978 69271 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69271 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21062990 64369 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64369 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798744 138943 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138943 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
11713742 93130 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93130 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44408013 74706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
44143499 187344 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
CHEMBL496815 187344 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
45272014 193648 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551543 193648 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
18435988 74534 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031725 74534 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
70695855 73129 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73129 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11613073 75577 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75577 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939881 64377 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818789 64377 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798680 138847 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 138847 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135486 91090 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91090 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
73356649 91100 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403870 91100 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
22421749 65974 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
CHEMBL184860 65974 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
11620005 81044 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81044 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397048 67098 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL188991 67098 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44442061 93923 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250730 93923 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
17545006 174664 5 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
CHEMBL4571855 174664 5 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
17173466 174671 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4572083 174671 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
44442093 93833 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL250311 93833 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
70693793 73207 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73207 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562416 176392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462352 176392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
45271103 193606 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551281 193606 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
70687478 73154 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73154 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
9848699 60314 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL176024 60314 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44417904 79967 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL214432 79967 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
71730661 122031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601374 122031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759544 130721 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686771 130721 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759585 130797 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686847 130797 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730916 130808 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686858 130808 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
10344176 66849 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66849 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25115856 60464 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761118 60464 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184696 121976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601037 121976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89690396 137724 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 137724 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71730661 122031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601374 122031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
1314 3670 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3670 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3670 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
11640515 80098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
20817762 76972 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 76972 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11640515 80098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
11975327 141229 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
CHEMBL386021 141229 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
44143494 183672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
CHEMBL483673 183672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
53318801 56407 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56407 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
49865679 15885 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 15885 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10250850 72066 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72066 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11419666 122038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
44394855 66944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 66944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
44405412 71530 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71530 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44417982 82100 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82100 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
89690239 137679 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 137679 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025110 137763 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 137763 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
89690292 137660 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 137660 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691193 138880 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 138880 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44403548 70049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
11656044 140606 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 140606 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10319824 66746 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 66746 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
44407710 73592 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73592 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70689596 73216 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73216 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695915 73220 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73220 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394973 65895 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184528 65895 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
122184570 121905 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600825 121905 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
22421750 70047 6 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194530 70047 6 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
91759582 130792 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686842 130792 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730790 130803 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686853 130803 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
71731049 130806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686856 130806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
16665072 98086 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98086 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
44417917 81684 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 81684 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
89690607 137649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 137649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184885 122030 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601373 122030 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
11419666 122038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
CHEMBL360142 122038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
11635187 194061 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557263 194061 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
18436123 74526 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
CHEMBL2031717 74526 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
44562564 188549 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 188549 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
56597991 138646 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 138646 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11511219 65804 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65804 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407991 168886 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168886 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394864 125677 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 125677 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
9955811 65840 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 65840 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394986 122822 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL361654 122822 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11452268 81161 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81161 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
54580457 60255 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60255 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
56673714 64389 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64389 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
22422406 67113 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
CHEMBL189083 67113 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
11583925 165218 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165218 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11342160 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360671 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11342160 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL360671 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44394972 65869 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184418 65869 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
22421743 66489 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL186077 66489 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
122184687 121968 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601024 121968 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
70687470 73114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442068 93925 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250746 93925 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
122184674 121935 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
CHEMBL3600982 121935 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
44407479 73315 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL201813 73315 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
11662657 80712 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80712 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
70685346 73150 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73150 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
86695564 130706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686756 130706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730532 130712 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686762 130712 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71731945 130729 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686779 130729 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759556 130739 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686789 130739 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730921 130741 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686791 130741 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732075 130743 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686793 130743 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
71730135 130758 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686809 130758 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759580 130790 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686840 130790 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759589 130809 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686859 130809 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
44417995 82029 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82029 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57402993 69290 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934825 69290 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70687552 73274 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73274 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89691439 137720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
11740891 121955 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601012 121955 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89691439 137720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3770359 137720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
90469437 120757 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120757 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438755 93070 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93070 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
45271829 193611 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551332 193611 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11634886 194990 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL564501 194990 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
18436125 74528 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031719 74528 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
11165058 154095 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154095 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
44562600 172560 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 172560 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11155432 82075 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82075 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
45267565 194611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562073 194611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11678370 136042 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136042 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44403484 70244 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194950 70244 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
49865790 15966 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 15966 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
59135479 91081 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403851 91081 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
15987638 126257 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
CHEMBL365374 126257 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
44562544 173269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
CHEMBL453886 173269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
49865708 15913 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 15913 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
91759577 130785 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686835 130785 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
57396022 69300 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934836 69300 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397820 69305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934840 69305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44143497 183530 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
CHEMBL482636 183530 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
45267739 194880 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
CHEMBL563791 194880 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
90666263 108886 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 108886 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
11531660 135071 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135071 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
12020156 194608 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL562016 194608 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
70685397 73217 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73217 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
127025110 137763 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 137763 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
70683237 73106 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73106 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44417942 82041 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217560 82041 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44401395 135463 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL373157 135463 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
90666254 108876 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 108876 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
44408099 75351 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204798 75351 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407950 140025 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL381143 140025 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
71717086 87360 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337753 87360 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
71714121 122034 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601377 122034 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
71730533 130788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686838 130788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
89690379 137652 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 137652 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89690318 137778 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 137778 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44193624 122015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601299 122015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691162 138841 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 138841 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
71660915 138883 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 138883 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273777 194179 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL558532 194179 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
44442121 93839 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
CHEMBL250326 93839 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
45270841 195058 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
CHEMBL565073 195058 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
11563017 80650 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80650 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11713027 80762 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 80762 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
23567290 63144 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179872 63144 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44405488 132491 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
CHEMBL370222 132491 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
44405488 132491 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
CHEMBL370222 132491 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
70695929 73268 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73268 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
21940052 64380 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64380 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
57401531 67810 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914855 67810 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
44397606 123554 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL363256 123554 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
90666253 108875 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 108875 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
71731943 130725 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686775 130725 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759547 130728 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686778 130728 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
11568782 71555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
11705485 167969 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 167969 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11511219 65804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11655872 71373 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71373 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
25115621 60445 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761099 60445 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
60130302 121846 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600390 121846 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
89691162 138841 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 138841 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691065 138931 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 138931 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
16739263 92981 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 92981 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11712898 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL472363 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23657037 94088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44442071 154077 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154077 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11712898 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11712898 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL472363 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 178609 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
44562500 186153 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186153 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
45487330 196975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL579232 196975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
11656489 15965 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223968 15965 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11511219 65804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70695917 73225 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73225 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44401508 69478 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL193666 69478 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
44401552 165353 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL425012 165353 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
11604236 176127 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL459897 176127 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
44388559 60395 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60395 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44402768 69459 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL193583 69459 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44442060 154269 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400297 154269 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44397454 123584 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL363337 123584 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44424070 85324 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85324 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
11520239 3575 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3575 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3575 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
44394698 65909 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 65909 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
10360874 64603 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64603 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
11662657 80712 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80712 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11554412 96573 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
CHEMBL266725 96573 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
10150955 80507 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80507 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 81888 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 81888 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141265 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141265 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71117 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71117 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25113835 60452 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761106 60452 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116082 60463 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761117 60463 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
16745235 121923 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600970 121923 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
122184695 121975 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601036 121975 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
127029624 137662 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 137662 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
57403784 68513 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68513 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
57890370 121892 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600812 121892 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184561 121895 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600815 121895 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11649549 93504 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93504 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11619850 75424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
CHEMBL204828 75424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
11619850 75424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
22348261 76710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 76710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
11775505 141455 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141455 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
44442053 154369 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400883 154369 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
24808474 91091 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91091 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952765 91096 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91096 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
71226964 128659 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 128659 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81154 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11598355 141271 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141271 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44397476 67088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
11553316 71290 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71290 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11340348 128938 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL367156 128938 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
44143503 187486 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497830 187486 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44408027 74717 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 74717 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
18436119 76029 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76029 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11222404 193708 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 193708 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487383 195307 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566662 195307 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
23593464 64371 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
58646147 78675 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 78675 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522945 76032 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76032 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
57522468 76041 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76041 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
1305 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
9934033 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
CHEMBL182150 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
11570040 77416 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL209109 77416 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10027853 71518 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71518 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23593464 64371 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23120540 194465 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 194465 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487652 198052 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL593521 198052 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
45487283 195795 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
CHEMBL569852 195795 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
45487309 196128 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572090 196128 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
21939950 64396 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64396 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44407710 73592 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73592 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407875 74712 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 74712 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436112 74498 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031578 74498 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
11583744 71380 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71380 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
127029623 137807 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 137807 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522950 76037 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76037 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
53321223 56424 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
CHEMBL1642487 56424 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
57399740 67742 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67742 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
71731807 130723 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686773 130723 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730394 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686824 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759584 130786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730659 130794 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686844 130794 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44405415 72224 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72224 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
44405486 139982 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 139982 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394860 65916 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 65916 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394606 66917 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 66917 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169096 87332 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337725 87332 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396019 69283 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934819 69283 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401250 69288 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934823 69288 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401252 69306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934841 69306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54584181 60451 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761105 60451 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70693807 73255 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73255 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690365 137647 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137647 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54585864 60321 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60321 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
21108118 67814 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914859 67814 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45273623 193961 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL556296 193961 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44143498 187201 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
CHEMBL495789 187201 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
45271642 193485 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550308 193485 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45487366 196104 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL571830 196104 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
6621104 66468 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL185997 66468 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
44397262 67168 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67168 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403480 70206 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70206 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403506 70790 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 70790 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403474 126705 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 126705 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403468 167866 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 167866 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
20779426 60225 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175874 60225 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
44417892 79826 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
CHEMBL213771 79826 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
71720118 87342 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337735 87342 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25114948 60470 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761125 60470 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
45267654 194407 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL560677 194407 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
9828622 96206 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
CHEMBL263702 96206 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
44397175 125867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL365094 125867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
11330800 81862 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL217132 81862 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11569340 71306 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71306 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562543 173267 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL453885 173267 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
70681117 73118 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73118 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44402593 71267 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196332 71267 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
44562499 186152 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488720 186152 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
44394774 66876 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187859 66876 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45272040 193437 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL549930 193437 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
71731944 130727 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686777 130727 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732077 130747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686797 130747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759583 130793 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686843 130793 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44424069 85303 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85303 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424071 141565 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 141565 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
70687551 73270 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73270 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117798744 138943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438747 92942 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 92942 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11974231 82008 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 82008 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
11511776 188711 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 188711 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11570031 73151 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73151 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408117 139029 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139029 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11778029 65877 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 65877 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
71717084 87352 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337745 87352 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44562542 172656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452335 172656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
11597758 193502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550455 193502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71731948 122014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601298 122014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759581 130791 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686841 130791 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
22254604 123358 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123358 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
25115173 60458 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761112 60458 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
70691738 73275 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73275 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11569300 82070 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82070 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
23022394 76027 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76027 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
59135478 91088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11296279 80139 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL214858 80139 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71719522 87340 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337733 87340 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
45268457 194464 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561133 194464 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
49865738 15940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 15940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417017 79970 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 79970 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397480 67034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
CHEMBL188655 67034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
44397215 67167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189492 67167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
44390752 122480 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360876 122480 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394925 65853 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184353 65853 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
137635978 155515 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 155515 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
70681116 73116 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73116 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666258 108880 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219267 108880 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
137635978 155515 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 155515 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
10353807 66017 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185096 66017 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
22427041 69968 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194417 69968 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
70689526 73160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408014 75042 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203929 75042 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71731948 122014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601298 122014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64393 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64393 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
122184566 121900 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600820 121900 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44407711 75579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
44442151 93572 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 93572 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44407944 165449 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165449 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11677277 141247 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141247 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
44405409 72055 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
CHEMBL198692 72055 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
45270147 193723 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL552010 193723 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11583925 165218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397636 66867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187814 66867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
49865977 16042 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16042 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11568741 194395 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560584 194395 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71226289 128669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670648 128669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
91759559 130744 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686794 130744 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732076 130745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686795 130745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730791 130805 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686855 130805 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
57396021 69293 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934828 69293 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690957 138795 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 138795 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691535 138852 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 138852 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
89691247 138878 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 138878 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44410878 77754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 77754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
45487392 195310 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566674 195310 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666098 108843 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 108843 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11454184 70745 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL195319 70745 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
71717700 87364 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337757 87364 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
59135490 91083 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403853 91083 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
11563153 136043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 79993 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79993 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
70691720 73206 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73206 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11705485 167969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 167969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44562479 186149 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488711 186149 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
10244148 65907 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
CHEMBL184573 65907 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
91759572 130774 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686825 130774 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71731047 130780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686830 130780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
91759584 130786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
11153928 165227 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165227 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
59835766 121904 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600824 121904 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89690864 138909 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 138909 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
86582974 120755 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 120755 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117816804 120756 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 120756 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
45270139 193627 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL551408 193627 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
11533195 194072 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557329 194072 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
18435984 74531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
CHEMBL2031722 74531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
11292322 153877 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398864 153877 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49865680 15886 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 15886 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 15941 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 15941 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44390733 62165 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL178084 62165 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
21939887 64378 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818790 64378 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44417960 81384 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL216429 81384 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
44394997 64225 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL181492 64225 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
1562 886 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
5312114 886 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL17645 886 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL195380 886 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
11974034 81685 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL216577 81685 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
70687537 73204 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73204 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
70691656 73161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442050 93812 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250118 93812 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
71731946 130735 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686785 130735 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759557 130740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686790 130740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
10466405 123359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362720 123359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44418009 81451 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81451 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
70683287 73224 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73224 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184564 121898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600818 121898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
86582974 120755 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 120755 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45271114 193693 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL551886 193693 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
70691650 73111 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73111 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184569 121903 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600823 121903 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
24952419 91098 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403868 91098 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10399494 66170 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL185235 66170 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11581666 75575 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
CHEMBL205106 75575 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
44143490 192077 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL521903 192077 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
11246373 93872 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250528 93872 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759558 130742 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686792 130742 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759560 130746 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686796 130746 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89690365 137647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54579973 60318 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60318 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89691247 138878 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 138878 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562563 173788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 173788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11555572 194529 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL561463 194529 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
44394939 65821 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184205 65821 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403454 71399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403445 165824 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 165824 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44424073 85198 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85198 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44417907 81060 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215989 81060 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44143489 187366 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL497005 187366 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
71226696 128673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670651 128673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
71731046 130711 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686761 130711 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
71731947 130737 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686787 130737 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
11589812 81150 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216180 81150 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
10126754 81145 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81145 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59691557 121927 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600974 121927 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
90469437 120757 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120757 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
117816748 138893 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 138893 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
71660914 138782 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 138782 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45272853 194060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557262 194060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
11634823 15963 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223966 15963 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44424067 142655 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 142655 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44390787 122050 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360159 122050 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394705 124801 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 124801 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11397595 124096 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL364071 124096 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
57392548 69298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934833 69298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
21939940 64379 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818791 64379 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939935 64382 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818796 64382 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690368 138966 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
CHEMBL3794523 138966 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
11591542 79993 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79993 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
20779429 60221 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL175860 60221 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
91759554 130736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686786 130736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89691535 138852 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 138852 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11974346 140968 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 140968 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11712583 193497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550410 193497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
11719912 194213 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
CHEMBL558928 194213 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
44442156 153854 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398748 153854 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11706442 194133 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL558052 194133 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127030071 138647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 138647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
127031356 138661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 138661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11440762 81729 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 81729 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
44403533 71112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44395021 65875 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184439 65875 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11974132 79795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
CHEMBL213658 79795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
44408013 74706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
70693796 73221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11464405 80085 18 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214731 80085 18 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11662657 80712 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80712 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11510399 81136 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216104 81136 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417847 82023 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82023 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417911 82027 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82027 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418002 82153 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82153 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10456755 70754 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70754 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114287 60250 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1760012 60250 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114067 60466 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761120 60466 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685409 73261 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73261 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184671 121931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600978 121931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184699 121980 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601040 121980 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
59835780 121965 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601021 121965 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835879 121967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
CHEMBL3601023 121967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
44438750 92980 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 92980 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11442761 139653 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
CHEMBL380429 139653 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
10075375 75649 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 75649 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
20817761 76915 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 76915 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
45268470 194621 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 194621 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
23120586 195062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 195062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
44143495 183673 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 183673 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
45270802 193408 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL549635 193408 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866036 16055 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16055 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44403517 71173 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71173 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
20817800 70074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
9910346 64401 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64401 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10050565 75353 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75353 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436120 74530 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74530 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
53322555 56413 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642474 56413 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
23022536 76031 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76031 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
11634230 69831 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69831 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23022509 76028 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76028 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417821 80147 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80147 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
57403785 68520 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68520 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23120512 193638 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 193638 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
57522704 76024 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76024 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
24780883 56419 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56419 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
45487284 195984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570987 195984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10173726 80433 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80433 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57396294 67746 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67746 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390750 63148 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL179878 63148 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
56666755 64391 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64391 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
45273703 194106 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557731 194106 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45487657 197315 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL585509 197315 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
44390778 63948 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL180962 63948 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
57392824 67741 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67741 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44407836 74916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11635274 138159 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377843 138159 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
44417999 81794 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 81794 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
23120564 194870 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563725 194870 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45271839 194872 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 194872 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
155531314 171046 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4465399 171046 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
45487391 197350 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL585879 197350 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
9807658 64215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181466 64215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
155538229 171803 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4476156 171803 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
91759543 130719 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686769 130719 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
44405645 72120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198890 72120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405468 132911 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 132911 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44405518 139829 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 139829 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394569 65885 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 65885 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11281523 81390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
44418010 81151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216184 81151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169097 87333 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337726 87333 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57390738 69276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934812 69276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57395050 68514 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68514 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
52917998 60308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683781 74601 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032047 74601 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
71660915 138883 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 138883 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45271111 193664 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551684 193664 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
45273401 194100 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL557715 194100 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
24952056 91087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
127031354 138575 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 138575 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627122 141206 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141206 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44407860 75070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407870 75561 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75561 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403467 70198 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70198 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403505 133047 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133047 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44402350 71684 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197571 71684 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
11678370 136042 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136042 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417824 141319 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386509 141319 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11410594 96753 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL268385 96753 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11562129 70733 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70733 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44394826 66272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10083869 65243 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11201645 71527 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71527 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
70687549 73263 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73263 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693808 73272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44193451 122013 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601297 122013 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691065 138931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 138931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143502 187400 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497221 187400 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562404 176390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
11706443 194549 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
CHEMBL561585 194549 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
44402484 133007 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL370839 133007 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11282448 62246 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62246 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
60168817 87346 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337739 87346 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690239 137679 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 137679 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44403547 133091 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371355 133091 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403500 134691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL372245 134691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44442054 93837 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250321 93837 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
45268644 194543 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL561546 194543 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
71716477 87351 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337744 87351 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11662564 133003 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 133003 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
137644041 157903 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157903 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
45269996 194747 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562905 194747 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
137644041 157903 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157903 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
25114064 60461 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761115 60461 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
89690318 137778 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 137778 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574358 178131 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468299 178131 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
44574359 178158 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468509 178158 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11634061 191755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 191755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
127033945 138424 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138424 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407991 168886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71225876 128670 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
CHEMBL3670649 128670 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
122184568 121902 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600822 121902 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
57394273 69296 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934831 69296 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44408013 74706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
137657882 159127 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159127 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
137657882 159127 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159127 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
11973798 79888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
CHEMBL214075 79888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
44143501 187399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
CHEMBL497220 187399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
44417910 82016 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL217435 82016 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417992 82045 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82045 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71588 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71588 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
117816804 120756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 120756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
89691032 138911 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 138911 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562442 178610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 178610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
155524512 170399 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
CHEMBL4455933 170399 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
44397033 66804 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187553 66804 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
702501 157042 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4080696 157042 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
22254575 65990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184980 65990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
10198125 126123 2 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365254 126123 2 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44403748 70281 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
CHEMBL194997 70281 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
11527169 77026 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL208635 77026 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
89691416 138930 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3794147 138930 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
45269336 194308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 194308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407956 74512 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74512 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11627085 193740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL552143 193740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44405517 71517 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197023 71517 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
71718319 87367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337760 87367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44403749 165668 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL426648 165668 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
45267386 194335 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560063 194335 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
71227161 128665 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
CHEMBL3670644 128665 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
44417848 141090 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141090 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
11516903 69937 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194253 69937 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
70681217 73273 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73273 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70693809 73276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89691032 138911 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 138911 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45487641 197351 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585880 197351 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
70691649 73108 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73108 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865653 15866 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 15866 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
57402500 67812 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
CHEMBL1914857 67812 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
46899579 16809 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253956 16809 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44402599 125664 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL364936 125664 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
52918017 60323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
57391045 67806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 67806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11419338 74097 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
CHEMBL202741 74097 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
45270303 194951 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL564243 194951 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
90666260 108882 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 108882 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
89691216 138871 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 138871 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11563153 136043 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136043 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417938 96889 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
CHEMBL269352 96889 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
89690379 137652 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 137652 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691144 138915 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 138915 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974131 141454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
70687473 73127 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73127 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184559 121887 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600808 121887 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
66877080 91099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403869 91099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
44394910 66672 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186947 66672 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44407967 74143 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74143 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
11591169 71402 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71402 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
44407667 74057 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74057 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
71731804 130720 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686770 130720 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71660914 138782 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 138782 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45268465 194886 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 194886 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18435986 74533 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031724 74533 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
11554989 178485 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 178485 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44407667 74057 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74057 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
57391030 67750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914648 67750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10258364 193116 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
44395022 165601 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL426252 165601 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44442069 154273 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400321 154273 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
91759575 123873 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3639387 123873 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
45272816 194116 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL557873 194116 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
70693732 73115 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73115 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44418008 81442 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL216454 81442 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44397278 66965 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188340 66965 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
22254580 66673 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186949 66673 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
44417963 165458 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL425445 165458 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
44405464 165798 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 165798 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44394856 65803 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 65803 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394824 123749 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 123749 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394611 123828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 123828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 123828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 123828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
16721015 80011 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80011 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11495432 97747 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL274168 97747 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018932 79896 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 79896 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018914 80503 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80503 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417956 96203 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96203 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
10388797 71415 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71415 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57392547 69291 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934826 69291 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25115855 60448 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761102 60448 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116079 60457 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761111 60457 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114722 60468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761123 60468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184563 121897 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600817 121897 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835728 121910 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600830 121910 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978428 121954 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601011 121954 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388351 121960 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601017 121960 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11408441 140724 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
CHEMBL383078 140724 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
44410823 75203 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75203 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348219 76171 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76171 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
20817821 76506 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76506 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410821 76770 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 76770 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11259253 82133 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82133 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
44442144 154157 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154157 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45270014 193443 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
CHEMBL549984 193443 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
45487372 195240 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566232 195240 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
9829942 65839 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
CHEMBL184291 65839 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
11236807 81154 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563017 80650 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80650 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11613073 75577 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75577 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44390715 123302 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362400 123302 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
53325164 56423 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56423 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
11752320 67390 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL190780 67390 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
57398088 67740 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67740 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45487390 195410 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL567514 195410 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
44394907 165439 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165439 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
23593464 64371 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23593464 64371 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939902 64388 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64388 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
44408108 139284 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139284 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57521366 76042 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76042 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407944 165449 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165449 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10186375 78538 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL2112988 78538 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
11683259 194093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557664 194093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45267577 194294 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 194294 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487331 197124 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL583348 197124 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10141528 122435 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL360731 122435 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
4219492 71093 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71093 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
56673713 66122 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66122 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66122 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
1314 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9865843 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
CHEMBL178707 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9978508 187457 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497637 187457 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522949 76036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
1314 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
9865843 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
CHEMBL178707 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
1314 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
9865843 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
CHEMBL178707 3670 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
56589628 67807 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67807 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
23120576 194105 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557730 194105 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11654412 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11654412 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 197240 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
57522947 76034 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76034 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
44407991 168886 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168886 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417944 141278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11502008 56278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11512135 69965 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69965 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
10024171 187462 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 187462 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
53317306 56411 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56411 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45487382 195721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL569458 195721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
59135482 91092 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91092 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44390706 121519 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL359510 121519 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11612403 71066 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195914 71066 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10185187 62969 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179325 62969 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
71730133 130752 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686803 130752 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
89798653 130783 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686833 130783 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
9806086 64876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 64876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
10434776 125861 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125861 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394959 66874 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66874 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405570 71648 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71648 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405408 72089 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72089 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405463 132636 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370361 132636 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
10083869 65243 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65243 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394859 65914 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 65914 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394573 123165 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123165 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
11591169 71402 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71402 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
60169184 87337 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337730 87337 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169263 87339 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337732 87339 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71719525 87358 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337751 87358 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
57396020 69292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934827 69292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394275 69302 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934838 69302 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54586089 60450 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761104 60450 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
56683679 64392 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64392 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44442135 153890 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398964 153890 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11511219 65804 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL184084 65804 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11496313 71968 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL198361 71968 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
59135471 91082 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91082 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11304816 65947 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
CHEMBL184717 65947 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
44397008 66568 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66568 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44397127 66748 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 66748 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44397026 126649 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 126649 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44403528 70201 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70201 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403499 70773 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 70773 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403522 123540 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 123540 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 124671 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 124671 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44442056 93871 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250527 93871 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44402549 71454 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196781 71454 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
70681213 73256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44438745 93425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
53325165 56425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642488 56425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
71716479 87365 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337758 87365 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397120 66555 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL186417 66555 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44403472 71385 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71385 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
155522708 170219 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4452982 170219 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44442100 154150 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
CHEMBL399712 154150 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
101007561 155848 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 155848 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
101007561 155848 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 155848 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44397099 66775 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
CHEMBL187413 66775 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
11510669 188710 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 188710 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
44394638 123282 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123282 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
49865869 16001 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 16001 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
86695569 130717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686767 130717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
91759546 130726 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686776 130726 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759563 130755 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686806 130755 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
22254582 66638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11973801 141436 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141436 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
10480652 64990 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 64990 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394607 123834 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 123834 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
70685395 73199 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73199 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
11599681 70001 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194484 70001 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54583209 60467 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761122 60467 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
91759590 130811 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686860 130811 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
70687538 73227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690607 137649 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 137649 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574357 178130 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468298 178130 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
44442097 93576 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 93576 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44394908 66873 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187850 66873 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
71720119 87353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337746 87353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
46899581 16825 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254141 16825 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11620005 81044 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81044 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 79993 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79993 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
44402419 71329 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196390 71329 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
45267385 193266 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL541944 193266 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
90666256 108878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 108878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
10083869 65243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695916 73223 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73223 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11270984 63437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL180168 63437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11270984 63437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
CHEMBL180168 63437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
5817261 69983 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194468 69983 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
25114065 60456 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761110 60456 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
59135485 91085 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403855 91085 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44403483 70033 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194521 70033 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44390456 64570 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
CHEMBL182235 64570 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
71716480 87366 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337759 87366 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11974233 81730 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 81730 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
49866087 16067 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16067 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
44408020 75081 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL204168 75081 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
91759588 122018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601302 122018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
54579974 3189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
91759588 122018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601302 122018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
11525369 140723 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
CHEMBL383076 140723 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
11974229 82071 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82071 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
45272837 194207 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558863 194207 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44442065 93875 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 93875 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24952417 91084 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91084 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44442066 93876 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250541 93876 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
71226436 128668 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
CHEMBL3670647 128668 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
91759574 130782 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686832 130782 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
11304816 65947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
CHEMBL184717 65947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
44442130 93757 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249714 93757 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44394684 126773 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL365876 126773 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
10353806 66570 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186481 66570 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44395001 65933 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184658 65933 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390369 64279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181727 64279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44402433 134695 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372291 134695 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
91759564 130756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686807 130756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759573 130781 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686831 130781 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
4219492 71093 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71093 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11974130 79952 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 79952 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394944 64544 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182161 64544 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
45267399 195009 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564674 195009 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
44405482 71507 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71507 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394792 124220 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124220 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
9799244 80173 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80173 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018997 141176 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141176 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57397819 69303 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934839 69303 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
122184693 121972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601033 121972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10433825 121885 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600806 121885 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
60130337 121894 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600814 121894 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9824856 121909 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600829 121909 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11504274 121952 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601009 121952 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
10024145 121956 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601013 121956 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11328029 76177 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
CHEMBL206081 76177 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
45273642 194781 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 194781 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
11599973 193228 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 193228 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
11599186 73152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56597407 138525 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 138525 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030069 138578 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 138578 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
11648912 79941 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 79941 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
44403467 70198 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70198 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403518 71420 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71420 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11560917 123534 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 123534 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10389978 69271 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69271 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44403765 135337 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135337 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
23593464 64371 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56666755 64391 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64391 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44408109 75192 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75192 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
127029624 137662 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 137662 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
45487673 195604 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568572 195604 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10344176 66849 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66849 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
21940008 64394 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64394 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57396294 67746 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67746 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44418003 82056 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82056 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
21108056 67738 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 67738 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18435980 74535 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
CHEMBL2031726 74535 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
11596311 56422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
57401509 67745 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67745 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44143496 191489 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 191489 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
53318593 56416 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56416 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
57522704 76024 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76024 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57522816 76030 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76030 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
155516949 169585 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4444299 169585 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71816518 137756 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137756 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
56680348 64390 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64390 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23120575 194200 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 194200 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
45487653 197329 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197329 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
53318594 56429 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642492 56429 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390768 64143 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181383 64143 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403765 135337 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135337 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
9824428 65925 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 65925 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394764 122653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 122653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
22254581 65893 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 65893 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44417856 80428 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80428 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169098 87334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337727 87334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169182 87336 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337729 87336 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25116309 60459 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761113 60459 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
11975438 79822 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 79822 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44397128 123583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 123583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44403501 69307 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69307 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44403524 71121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11611530 134282 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134282 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
89691216 138871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 138871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44401671 69923 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194173 69923 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10466478 123510 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL363011 123510 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695918 73228 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73228 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57390252 67811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 67811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
45273659 194159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 194159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44442124 154354 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400799 154354 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11583925 165218 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165218 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563153 136043 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136043 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44402414 71062 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195896 71062 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
10443853 65884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184476 65884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45270273 193914 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL555349 193914 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
70689594 73200 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73200 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
127025395 137753 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 137753 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
57399742 67751 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914651 67751 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9999058 93870 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250526 93870 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
70693794 73211 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73211 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
70685398 73229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45273783 194193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558726 194193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
45273790 194248 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL559329 194248 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
59135479 91080 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403850 91080 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44407967 74143 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74143 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
10389430 125430 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL364863 125430 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
59691584 121929 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600976 121929 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
70687479 73163 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73163 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562481 185429 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL487041 185429 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70695860 73069 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016580 73069 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56683679 64392 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64392 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44438742 93392 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247689 93392 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11374857 79809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 79809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
44394921 65908 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 65908 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
44394961 66899 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL187953 66899 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
10038053 65777 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183932 65777 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
53321222 56417 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642478 56417 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
49865975 16039 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16039 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10456755 70754 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70754 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
117798675 138830 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 138830 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
71660917 138844 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 138844 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11464405 80085 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80085 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
44250211 194548 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL561584 194548 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127029632 137794 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 137794 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
53317524 56420 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642483 56420 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
17484866 66506 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
CHEMBL186159 66506 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
90666261 108884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 108884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70681215 73265 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73265 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11975326 80097 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80097 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
45270319 193551 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550816 193551 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44562565 173499 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL454424 173499 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
45272539 194237 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
CHEMBL559237 194237 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
44394587 123547 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363220 123547 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
22421739 66780 6 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL187430 66780 6 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
86695565 130707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686757 130707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759584 130786 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130786 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759578 130812 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686861 130812 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45270850 194979 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL564413 194979 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
59135474 91093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
70695913 73202 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73202 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44401368 69916 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL194122 69916 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
49866086 16066 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16066 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70685410 73264 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73264 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
60130349 121881 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600802 121881 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44410904 171890 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171890 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442063 93959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 93959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
49865678 15884 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 15884 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
44403478 165760 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427187 165760 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44388096 63180 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
CHEMBL180009 63180 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
70685408 73258 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73258 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
127028868 138812 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3792826 138812 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
70691648 73104 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016699 73104 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44407989 75030 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203858 75030 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
44405619 72159 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72159 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44394725 65820 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 65820 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
11719291 81486 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216482 81486 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
11711452 81624 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216554 81624 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
57394274 69299 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934834 69299 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25116307 60454 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761108 60454 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
16742746 121933 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600980 121933 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10274635 68517 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68517 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
122184832 122010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601294 122010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
9978490 121908 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 121908 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44410838 76708 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 76708 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
53324076 56415 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56415 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
44442064 154270 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154270 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
45487384 195166 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 195166 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
70681113 73109 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73109 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691653 73134 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73134 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
71226400 128661 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 128661 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 138538 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 138538 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71226277 138589 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 138589 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81154 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11641948 79931 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79931 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
11583747 81083 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81083 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
44403524 71121 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71121 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11603897 123809 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 123809 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11548234 70852 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70852 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45271907 193386 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL549512 193386 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44408028 140373 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140373 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57391028 67743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 67742 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67742 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
21062998 64384 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64384 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690574 137797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57392824 67741 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67741 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11532924 137854 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 137854 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
89690574 137797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53317307 56418 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56418 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
127029623 137807 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 137807 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522701 76043 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76043 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
71226895 128666 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
CHEMBL3670645 128666 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
91759552 122017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3601301 122017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759551 130733 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686783 130733 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
44394909 66699 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 66699 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44405519 72026 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72026 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394605 66683 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 66683 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394639 66373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10361342 122409 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122409 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11188955 80057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
60168816 87344 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337737 87344 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759552 122017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601301 122017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64393 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64393 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798671 138826 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 138826 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
57401508 67744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 67744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
44403516 69951 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 69951 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403480 70206 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70206 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403479 97756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 97756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403538 135588 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 135588 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403479 97756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 97756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403511 135650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 135650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
122184567 121901 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600821 121901 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11409615 141233 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL386039 141233 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
91759576 130784 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686834 130784 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
11178792 94089 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251702 94089 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45268247 194920 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564032 194920 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
44407629 168089 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168089 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11304816 65947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL184717 65947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
44394998 64842 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182466 64842 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11676200 178636 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472554 178636 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71718911 87369 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337762 87369 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759565 130759 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686810 130759 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
89690124 137771 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 137771 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691143 138785 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 138785 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44395019 65905 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65905 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
60168914 87345 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337738 87345 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
22254540 66718 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL187165 66718 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
44407870 75561 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75561 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
89691144 138915 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 138915 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974230 165459 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 165459 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
18436129 74527 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
CHEMBL2031718 74527 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
44394596 65873 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 65873 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
22421743 66489 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186077 66489 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
70695852 73120 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016716 73120 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11546687 81143 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81143 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
25115852 60446 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761100 60446 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70681214 73259 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73259 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117816748 138893 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 138893 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
11635332 193403 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL549595 193403 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
25116306 60453 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
CHEMBL1761107 60453 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
11975436 78683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 78683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
11632909 132920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 132920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417898 82163 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL217860 82163 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
10202381 68516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44417890 165423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL425257 165423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
21939767 64367 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64367 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
89691019 138863 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 138863 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117816753 138807 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 138807 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798780 138861 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 138861 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135492 91095 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91095 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16721015 80011 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80011 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
54583954 60311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10386529 121958 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601015 121958 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
71660917 138844 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 138844 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
57396310 67808 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914853 67808 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
89690600 137651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 137651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
59835909 121961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601018 121961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11351174 139596 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL380144 139596 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11526309 188629 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 188629 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
11396908 71468 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL196839 71468 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
70695851 73105 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73105 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
10443307 66612 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186659 66612 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
86695566 130708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686758 130708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
57401508 67744 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 67744 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
70689525 73159 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73159 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
10303307 64145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181393 64145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10073563 67195 5 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL189653 67195 5 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44394931 123519 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL363047 123519 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11531010 133065 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133065 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
15133403 204627 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 204627 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25113838 60460 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761114 60460 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184558 121884 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600805 121884 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184560 121888 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600809 121888 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
59835725 121911 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600831 121911 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835758 121966 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601022 121966 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
23593464 64371 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64371 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
45271633 193873 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL554511 193873 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666097 108842 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 108842 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11591644 15914 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 15914 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522945 76032 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76032 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
44403517 71173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
10436090 65874 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 65874 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
57401510 67748 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 67748 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45272701 193978 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL556432 193978 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
1305 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
9934033 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
CHEMBL182150 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
57522946 76033 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76033 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57522701 76043 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76043 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
23593474 64372 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64372 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939915 64385 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64385 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
57398088 67740 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67740 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11582824 77739 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 77739 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
56673713 66122 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66122 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66122 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57401509 67745 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67745 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44402329 71578 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL197210 71578 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11563383 70171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
71730269 122020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601304 122020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
53317305 56410 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56410 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
24952419 91094 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91094 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44143504 187487 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497831 187487 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45487653 197329 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197329 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
44394572 66181 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66181 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394883 125843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 125843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169185 87338 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337731 87338 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60168818 87347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337740 87347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71720120 87356 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337749 87356 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690600 137651 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 137651 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
57390252 67811 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 67811 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
44442148 154158 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399734 154158 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44403472 71385 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71385 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
44417915 140857 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 140857 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
11632484 69991 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 69991 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
44407711 75579 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75579 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
22254570 65809 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184102 65809 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
70683299 73260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45271994 193517 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL550535 193517 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
44401616 69690 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193970 69690 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
45273392 194067 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
CHEMBL557306 194067 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
10421932 66747 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187295 66747 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417934 82053 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL217605 82053 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
11496313 71968 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71968 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
3611477 126992 7 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL366180 126992 7 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89690124 137771 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 137771 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
45272024 193741 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
CHEMBL552144 193741 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
44562415 176391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44408109 75192 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75192 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402505 71099 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196115 71099 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
44396196 66651 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186842 66651 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
10083101 65739 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183739 65739 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
89789910 130713 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686763 130713 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45267561 194910 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL563984 194910 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407711 75579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
11204090 63177 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL180003 63177 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401449 70750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195346 70750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
10149893 81041 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215955 81041 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
91759555 130738 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686788 130738 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
23593472 64374 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64374 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70691651 73117 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73117 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442067 93877 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250544 93877 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
1314 3670 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3670 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3670 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11539632 70217 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70217 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89691057 138941 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 138941 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
10255474 123154 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123154 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44405477 71669 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197485 71669 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691724 73222 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73222 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44207909 16520 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16520 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16520 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16520 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
57391027 67737 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914628 67737 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391045 67806 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 67806 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44438753 93027 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93027 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
49865871 16003 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 16003 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44407956 74512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417976 165389 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165389 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
49865976 16041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44395082 65755 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL183839 65755 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
44442119 93814 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250122 93814 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
155520135 172672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
CHEMBL4524539 172672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
59691661 121930 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600977 121930 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730269 122020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3601304 122020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44405651 71586 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71586 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
44417844 141055 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141055 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141129 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141129 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25116308 60455 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761109 60455 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
122184697 121977 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601038 121977 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
9934161 74602 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032048 74602 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44410904 171890 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171890 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442090 93726 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 93726 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
44442139 94022 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94022 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693733 73128 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73128 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16068 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16068 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
127030367 138534 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 138534 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 138631 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 138631 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597689 138636 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 138636 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11627122 141206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44403477 71484 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71484 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403513 133756 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 133756 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403511 135650 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 135650 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403518 71420 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71420 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11545677 70034 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70034 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
89689924 137804 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 137804 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89702566 138798 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 138798 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11512135 69965 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69965 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44390742 122774 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL361442 122774 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11559625 56421 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56421 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390713 123178 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362193 123178 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44573820 192665 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL523882 192665 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11627530 75557 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75557 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10005009 165823 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165823 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
56666754 64383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44573932 186908 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
CHEMBL494156 186908 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
22254551 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
44394592 65431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
22254551 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
22254551 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 124524 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
71719526 87361 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337754 87361 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89691284 138892 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 138892 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117798671 138826 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 138826 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798692 138816 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 138816 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45273778 194180 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558533 194180 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23022394 76027 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76027 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44396952 66395 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66395 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397425 66543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
44397221 66796 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 66796 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44403527 126654 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 126654 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403498 70734 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 70734 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
57403264 67734 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914625 67734 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
89691264 138957 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794445 138957 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143505 187458 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497638 187458 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562405 190313 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518514 190313 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
57390739 69297 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934832 69297 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691739 73277 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73277 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11974228 79962 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 79962 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
44407860 75070 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75070 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402567 165259 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL424836 165259 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
44394983 65948 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 65948 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
122184700 121981 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601041 121981 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
89690237 137696 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 137696 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44562403 189236 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189236 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
46902026 16790 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253789 16790 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44562462 178589 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472196 178589 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
91759550 130732 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686782 130732 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683300 73262 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73262 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
59691704 121928 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600975 121928 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
127025395 137753 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 137753 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
44407997 75038 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL203917 75038 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
44413259 139160 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
CHEMBL379802 139160 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
44417906 140878 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL384043 140878 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
44417864 79880 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 79880 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44403747 70242 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194946 70242 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
122184691 121969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601030 121969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89690622 137808 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 137808 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21939767 64367 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64367 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
127029631 137684 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769964 137684 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57401251 69289 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934824 69289 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70685336 73107 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73107 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394926 125739 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365011 125739 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390385 122001 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360117 122001 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417955 82022 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217460 82022 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
44562443 178611 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
CHEMBL472380 178611 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
11705240 132292 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132292 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
20817864 75707 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 75707 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
44402635 71510 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL196991 71510 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
127028869 138965 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3794501 138965 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
11974227 168739 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 168739 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
11635230 193903 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL555135 193903 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
127029632 137794 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 137794 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442070 154088 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399312 154088 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11520239 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
1313 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
CHEMBL185271 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
45273336 194089 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 194089 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 194089 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
45273336 194089 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 194089 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 194089 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
9915039 60498 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL176219 60498 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
10258364 193116 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
11520239 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
1313 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
CHEMBL185271 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
11520239 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
1313 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
CHEMBL185271 3575 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
45279585 123066 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123066 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
10118862 60478 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176159 60478 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
4033 1868 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1868 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1868 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
45279585 123066 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123066 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
45279490 123060 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123060 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10230490 62849 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178997 62849 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10258364 193116 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10118863 60494 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176208 60494 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44455336 95145 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
CHEMBL257733 95145 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
45279490 123060 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123060 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
45278579 123061 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123061 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10258364 193116 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193116 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193116 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
16043291 79583 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79583 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10004545 74603 4 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74603 4 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10324628 141693 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 141693 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 166809 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 166809 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
10209344 122738 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL361392 122738 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44416651 79987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 79987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416651 79987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 79987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
45278579 123061 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123061 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
46188603 121250 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121250 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
45279869 123070 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123070 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
10204151 165335 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL424961 165335 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10114686 60246 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175993 60246 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141308 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141308 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10186594 167996 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL435708 167996 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10226765 122620 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
CHEMBL361215 122620 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
10226765 122620 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL361215 122620 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141308 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141308 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430458 142279 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142279 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
11719447 66648 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL186827 66648 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397114 127028 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL366309 127028 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
11640865 77417 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209110 77417 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532402 138766 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379189 138766 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
10204047 60195 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175709 60195 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10231341 63016 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL179437 63016 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
11582824 77739 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 77739 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44424218 165492 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425654 165492 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52948857 18975 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
CHEMBL1289614 18975 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
10113523 129294 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL367532 129294 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11661999 77139 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208720 77139 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
10117415 60499 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176220 60499 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10298251 130853 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL368888 130853 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414520 79861 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 79861 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279869 123070 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123070 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
45279867 123085 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618363 123085 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
10369833 92135 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92135 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
10161039 60211 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175815 60211 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11307645 81716 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216681 81716 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11582825 78179 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL211223 78179 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
45279148 123076 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123076 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416800 96394 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96394 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 168805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 168805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 168805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 168805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44413240 79407 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
CHEMBL212053 79407 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
44414497 178565 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 178565 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 178565 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424212 85326 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229113 85326 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424213 85330 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229171 85330 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
10174940 140561 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382668 140561 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
10301472 124136 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364162 124136 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
11519451 139686 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL380509 139686 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
11635674 200164 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200164 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45279402 123072 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123072 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
10437982 92139 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92139 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
10183297 92880 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 92880 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
11168186 67686 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
CHEMBL191393 67686 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
44416859 140995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 140995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11612046 77431 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209172 77431 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532214 138106 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377588 138106 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424215 136661 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374844 136661 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16755871 92063 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92063 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16755870 143953 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 143953 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756284 150954 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 150954 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
11168831 123518 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL363044 123518 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
44416859 140995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 140995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416670 141392 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141392 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
49869631 127579 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665347 127579 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
58093389 127612 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665379 127612 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
49870047 127638 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665404 127638 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
49868914 129282 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129282 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092307 129291 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675316 129291 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
44424062 85433 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229791 85433 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44455368 95186 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95186 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416970 79918 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 79918 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80100 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80100 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416898 140933 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384282 140933 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11719647 138378 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378309 138378 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44414518 77556 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77556 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 79771 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 79771 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
9986044 80434 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215259 80434 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16739324 149227 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149227 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44397031 126259 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL365400 126259 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425810 142885 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389809 142885 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
9985634 79347 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79347 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424214 85331 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229172 85331 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
11511671 140677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382841 140677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756185 149189 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149189 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756641 142057 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142057 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49868672 127542 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665310 127542 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
49868941 127552 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665320 127552 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49869071 127554 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665322 127554 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424195 85440 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229822 85440 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44415364 79422 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79422 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
50903065 131303 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131303 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
49869490 127573 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665341 127573 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
11752339 69056 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69056 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
49869347 127567 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665335 127567 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
10053937 79838 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 79838 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869493 127577 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665345 127577 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
44425828 165740 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL427107 165740 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756405 92435 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92435 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
10139873 79696 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213198 79696 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
23567513 62065 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177955 62065 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
44417830 80178 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
CHEMBL215005 80178 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
44415419 79380 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
CHEMBL211934 79380 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
44440593 148563 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394311 148563 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44416797 80192 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL215075 80192 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
21101416 141357 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386753 141357 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020151 193518 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550545 193518 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44440587 93214 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246790 93214 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389461 122110 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360327 122110 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
44416474 79980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214499 79980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
57524677 125892 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
CHEMBL3651089 125892 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
44389521 64232 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
CHEMBL181516 64232 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
57524582 125872 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651069 125872 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
45271219 193759 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
CHEMBL552292 193759 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
45279491 123058 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123058 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45271221 193792 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552498 193792 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
12020161 193143 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL538968 193143 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
44416310 96210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
CHEMBL263771 96210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
44437544 151195 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396448 151195 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437544 151195 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396448 151195 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
23567394 60549 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176230 60549 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
44415501 77591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44440588 93162 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246590 93162 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389533 171870 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL447835 171870 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
20779413 60242 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175964 60242 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
20779393 123054 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL361821 123054 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49868664 129141 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673560 129141 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
49870454 127603 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665370 127603 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870576 127615 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665382 127615 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
58093397 127622 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665389 127622 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
58093339 127623 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665390 127623 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
49870706 127631 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665398 127631 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
49869331 129262 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675289 129262 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
44417905 82060 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82060 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44416970 79918 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 79918 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11546697 77013 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208551 77013 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
11758076 79634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212941 79634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
9851676 138010 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377519 138010 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415364 79422 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79422 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
10053937 79838 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 79838 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
46869326 65139 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830042 65139 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
56680482 65142 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830045 65142 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424217 85338 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229223 85338 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424186 165495 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425664 165495 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52942795 18978 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289619 18978 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
52941615 18994 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289722 18994 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
25205317 19121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290593 19121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11605821 141059 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL385011 141059 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11420543 67101 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL189029 67101 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
49869208 127561 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 127561 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
25054289 18895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289054 18895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
49868940 127551 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665319 127551 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
11785761 140868 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383976 140868 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11785261 67243 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL190068 67243 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
57988809 80089 10 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL2147472 80089 10 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
49869775 127582 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665350 127582 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49868805 127544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665312 127544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
49869488 127557 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665325 127557 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
50902183 124105 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640814 124105 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
44416840 141318 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL386507 141318 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44388277 62976 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179345 62976 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415501 77591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44425792 85523 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL230082 85523 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
44388141 60178 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175581 60178 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49869916 127591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665359 127591 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
11635674 200164 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200164 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
1252415 154084 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
CHEMBL399302 154084 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
11238718 160947 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL412801 160947 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44414465 167812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL434571 167812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416357 165519 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425791 165519 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44425795 85524 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL230083 85524 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44416587 140884 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL384079 140884 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44424263 85360 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229406 85360 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
10311260 66926 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL188084 66926 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
45267849 194458 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL561092 194458 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
71450908 78539 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL2112989 78539 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
10483604 79426 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212142 79426 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
2881764 94137 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
CHEMBL251947 94137 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
49870184 127593 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665360 127593 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
66886358 127607 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665374 127607 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
58093414 127648 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665414 127648 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
49869049 129260 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675287 129260 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
49869051 129261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675288 129261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
49870810 129270 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675296 129270 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868783 129272 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675298 129272 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
58092273 129288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675313 129288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
66608367 124101 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640808 124101 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
50901935 131315 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694007 131315 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44397309 67188 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL189602 67188 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44417861 80214 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215113 80214 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424063 141541 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387989 141541 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
44388293 62955 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179260 62955 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425832 150944 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396221 150944 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
10257135 141119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424211 136660 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374843 136660 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279680 123071 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123071 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
45279871 123077 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123077 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279064 123078 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123078 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
25054804 18980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289623 18980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
49869492 127575 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665343 127575 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
49870553 129246 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129246 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
10257135 141119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
11295707 167659 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL433591 167659 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416786 79889 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 79889 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
52947616 18947 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289399 18947 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44414368 141401 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL387055 141401 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424073 85198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44437542 151193 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396447 151193 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437542 151193 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396447 151193 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
52947578 16864 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254556 16864 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
58092293 129895 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680177 129895 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
11610423 165466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
23567355 62078 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177981 62078 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
23567432 122104 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360303 122104 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
49868666 129140 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673559 129140 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
45278576 123069 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123069 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
2729098 80084 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80084 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
44417865 97740 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL274102 97740 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416559 79475 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212344 79475 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989356 168354 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL438637 168354 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416928 80187 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215040 80187 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
52947297 19035 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290045 19035 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44388219 62959 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179275 62959 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49869915 127590 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665358 127590 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
58093398 127621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665388 127621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
49870183 127635 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665401 127635 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
49869917 127636 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665402 127636 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
49869186 129264 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675290 129264 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL4115718 211157 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44417855 80980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL215934 80980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
44414319 141329 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386552 141329 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414392 79788 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 79788 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10347754 82046 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL217581 82046 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388289 62759 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178882 62759 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425809 96674 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL267690 96674 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44415389 80943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 80943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424253 85342 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229230 85342 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11634329 141768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL388524 141768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
10238912 75627 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75627 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
11627316 140031 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381162 140031 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
10312052 140789 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL383432 140789 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
58423512 123064 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123064 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279871 123077 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123077 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45278578 123082 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123082 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
58423512 123064 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123064 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205152 19144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290712 19144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
44415389 80943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 80943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
49868938 127549 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665317 127549 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131306 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131306 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
49868676 127555 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665323 127555 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
11489588 80460 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215277 80460 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388427 63012 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179417 63012 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
23567283 62935 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179152 62935 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11656728 81860 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217114 81860 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
49868674 127545 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665313 127545 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
50901934 131314 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694006 131314 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44424166 85492 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229929 85492 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44417833 81752 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216964 81752 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
45272120 194794 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563223 194794 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44416833 141063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385038 141063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424174 85377 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229556 85377 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
23567477 60186 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175653 60186 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44417881 79988 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214516 79988 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416839 80703 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215635 80703 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
49868937 127548 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665316 127548 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
44414522 96410 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL265365 96410 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10436862 79423 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212136 79423 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347753 80223 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215118 80223 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
45271246 193537 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550683 193537 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44414651 136707 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL375132 136707 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11340894 134067 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
CHEMBL371809 134067 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
49870457 127613 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665380 127613 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
49870809 129269 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675295 129269 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868781 129284 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675309 129284 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49868782 129285 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675310 129285 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902181 124108 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640817 124108 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
50903066 131305 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131305 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL4115726 211158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416786 79889 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 79889 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
11641550 139203 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379829 139203 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
71714121 122034 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122034 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
44414357 79343 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79343 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430493 86581 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232438 86581 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44430500 86792 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232835 86792 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
9986014 141300 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386411 141300 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388294 63541 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL180364 63541 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397302 66607 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL186642 66607 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44415461 79891 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 79891 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415524 140685 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 140685 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44389404 121963 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360102 121963 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279772 123067 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123067 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
52941152 18995 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289723 18995 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
52947251 19009 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289830 19009 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
52941195 19021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289946 19021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
25017298 19109 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290493 19109 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16755970 91882 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 91882 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
44415524 140685 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 140685 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11467626 159261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL410566 159261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
49868803 127541 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665309 127541 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
44415461 79891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 79891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869073 127558 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665326 127558 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
49870553 129246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
44388263 165238 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL424784 165238 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
16756640 92846 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 92846 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
44416475 79997 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214547 79997 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45266975 193106 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
CHEMBL538211 193106 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
44417876 141190 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385743 141190 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
44416737 80083 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214717 80083 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44424203 165497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL425669 165497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44389484 62643 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178515 62643 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
44430490 86387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232231 86387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44437612 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437612 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437558 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437612 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437558 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437612 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91124 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91320 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437495 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44437495 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91468 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44424260 85351 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229348 85351 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
49868936 127547 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665315 127547 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870051 127642 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665408 127642 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
45267827 194561 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561694 194561 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
44437609 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437609 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90530 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
49868668 129143 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673562 129143 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
58079421 129144 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673563 129144 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
66873457 127627 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665394 127627 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
66873578 127629 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 127629 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
57524507 125871 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651068 125871 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
57524583 125873 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651070 125873 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
66603668 129293 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675318 129293 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL4115747 211165 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414606 96286 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL264350 96286 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10348080 79390 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211984 79390 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347752 80683 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215567 80683 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430482 87935 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234930 87935 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44424171 85374 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229505 85374 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424179 85382 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229609 85382 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424182 85394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229664 85394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424255 141818 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388723 141818 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424181 142246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389274 142246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424185 168402 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL439013 168402 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44409479 74668 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
CHEMBL203388 74668 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
11699265 76379 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206637 76379 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
45279772 123067 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123067 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
45279321 123080 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123080 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45278578 123082 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123082 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45278577 123083 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123083 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194383 19107 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290491 19107 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25205149 19019 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289941 19019 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
137640352 156254 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL4071004 156254 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
16072132 80017 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214629 80017 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44414464 96372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL265089 96372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44409527 74523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL203166 74523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
50903065 131303 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131303 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44417069 141381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
17989369 141237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386050 141237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10139496 168772 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL441855 168772 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44397323 66809 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187563 66809 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425796 85676 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231044 85676 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425821 142890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389811 142890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425801 85707 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231147 85707 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
49870683 129257 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675284 129257 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
44430481 150621 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395957 150621 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
20779441 63143 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179869 63143 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
45272111 193545 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550744 193545 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44416585 79860 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213923 79860 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416389 138124 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL377658 138124 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
58093337 127624 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
CHEMBL3665391 127624 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
58092304 129290 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675315 129290 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
58092269 129889 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680171 129889 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
44424061 85423 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229739 85423 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44417069 141381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414570 77685 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 77685 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
10008279 79388 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211978 79388 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10100662 140896 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384115 140896 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10461033 140910 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384163 140910 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388303 62221 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL178250 62221 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
44397350 124904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL364573 124904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
44425834 150884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 150884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415413 137848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 137848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
44424177 141471 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL387501 141471 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
25206616 18792 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1287838 18792 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
50903066 131305 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131305 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44415413 137848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 137848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
11168108 80009 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214583 80009 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415483 95968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 95968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869208 127561 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 127561 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
11656805 141312 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL386487 141312 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11648976 139806 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL380692 139806 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
11541231 140627 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL382772 140627 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
49870324 127596 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665363 127596 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
44388271 62648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178549 62648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
15982955 93215 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246794 93215 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
23567310 167936 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL435329 167936 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
44437614 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
11786476 66897 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187942 66897 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
44437614 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 144604 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
25018075 19151 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290722 19151 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44416381 79738 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213383 79738 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44194482 19088 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290381 19088 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
44417885 80193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215078 80193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437541 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
49869779 127586 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665354 127586 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
58093367 127637 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665403 127637 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
57524675 125882 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
CHEMBL3651079 125882 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
66603581 129891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680173 129891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
58092191 124098 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640805 124098 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
50901932 131312 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3694004 131312 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
44417862 80219 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80219 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
44414650 79790 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213649 79790 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44430478 86825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 86825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
44430452 149226 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149226 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
44430485 150911 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396193 150911 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415483 95968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 95968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11691468 168778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL441886 168778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
45278577 123083 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123083 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
52947270 19020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289945 19020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
49870553 129246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129246 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
25054550 19010 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289833 19010 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
49869489 127572 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665340 127572 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
49869632 127580 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
CHEMBL3665348 127580 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
44417837 140870 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383981 140870 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
44437541 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 145549 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
11445353 84717 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
CHEMBL224943 84717 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
3747253 94161 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
CHEMBL252145 94161 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
44437622 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437622 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 90945 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
45267809 194364 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560290 194364 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49870681 129251 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675279 129251 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44440599 146174 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL392403 146174 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
49870182 127644 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665410 127644 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44417841 81178 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81178 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44416782 80027 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80027 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44414455 79862 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 79862 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
44430498 87931 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234920 87931 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44424246 137038 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL375465 137038 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11655701 138179 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL377955 138179 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389403 62697 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178810 62697 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45278977 123065 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123065 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279680 123071 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123071 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
16756639 92798 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 92798 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
10195667 134765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
CHEMBL372721 134765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
44415533 79572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 138805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 138805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425827 150378 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395763 150378 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415512 79940 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 79940 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
11504793 81158 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216209 81158 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397145 67050 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188766 67050 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10077022 16872 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254630 16872 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44424225 85350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229339 85350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44415512 79940 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 79940 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
45270416 194978 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL564409 194978 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44388058 165467 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
CHEMBL425521 165467 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
44437497 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437497 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91559 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424167 141582 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388302 141582 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
67970877 125891 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
CHEMBL3651088 125891 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
49868917 129267 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
CHEMBL3675293 129267 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
49868914 129282 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129282 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092290 129286 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675311 129286 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902100 124110 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640819 124110 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
50903067 131306 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131306 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44424069 85303 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85303 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424064 85434 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229792 85434 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44414499 79917 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 79917 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
44430496 86688 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232634 86688 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397167 66902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL187968 66902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44425825 150669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395986 150669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415533 79572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 138805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 138805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
25205827 19064 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290262 19064 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
11247985 67684 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL191390 67684 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
44416782 80027 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80027 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44415526 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416714 140922 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 140922 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10300618 77975 12 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL2110360 77975 12 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
9954518 79618 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL212890 79618 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
10225681 79928 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214276 79928 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
17989329 80669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215508 80669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
16046114 141378 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386925 141378 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10159797 165426 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL425263 165426 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44397126 123755 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363479 123755 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11612847 81883 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
CHEMBL217182 81883 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
12020164 194080 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557473 194080 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416224 138968 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379457 138968 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
49869190 129280 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675305 129280 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
44424065 85435 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229793 85435 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
44416713 80054 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214667 80054 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45267812 194408 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560689 194408 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44424262 85352 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229350 85352 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
44416910 80104 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214790 80104 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
11387603 123748 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL363459 123748 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416711 80274 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215141 80274 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416579 80696 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215614 80696 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416817 168757 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL441696 168757 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
11569327 165451 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL425410 165451 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416881 81995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 81995 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416800 96394 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96394 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11635674 200164 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL607121 200164 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11560835 139353 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379933 139353 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44414451 168373 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168373 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430460 86798 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 86798 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
11520239 3575 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
1313 3575 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
CHEMBL185271 3575 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
44396807 66765 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187371 66765 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
44397630 67033 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188654 67033 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397288 67107 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189043 67107 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
44397479 121535 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL359580 121535 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44424196 85441 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85441 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11569327 165451 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL425410 165451 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81154 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10165163 127984 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL366703 127984 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44414475 77721 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 77721 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424190 165621 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL426369 165621 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44388215 60394 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176079 60394 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10224210 62981 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179353 62981 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11353174 80185 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215030 80185 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416670 141392 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141392 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10128900 140370 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382140 140370 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756754 91697 21 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 91697 21 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
11610423 165466 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165466 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
44424244 85332 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229177 85332 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11577410 76376 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206616 76376 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279402 123072 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123072 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45279868 123074 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123074 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
44416877 140862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 140862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
44481640 65146 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
CHEMBL1830049 65146 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
44424196 85441 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85441 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424256 168233 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL437544 168233 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279148 123076 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123076 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
50908739 18893 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289051 18893 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
10325618 92056 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243128 92056 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
10273126 60818 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176548 60818 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44417879 79973 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214470 79973 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
11584710 140769 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL383340 140769 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11524613 138703 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378869 138703 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44481905 65147 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830050 65147 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
10289615 76914 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL208025 76914 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
11584710 140769 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL383340 140769 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44417024 79979 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 79979 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416881 81995 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 81995 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416877 140862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 140862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10142124 60204 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175783 60204 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10164110 128953 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367215 128953 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414600 138997 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379535 138997 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11626170 78786 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
CHEMBL211340 78786 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
45279493 123062 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123062 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
24857598 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
24857598 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289283 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
50908738 19149 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1290720 19149 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
24857598 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289283 18929 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10165503 125432 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364871 125432 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
10115919 63028 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179493 63028 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11238080 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL205285 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414622 77734 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL210155 77734 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44424188 85422 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229716 85422 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11238080 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205285 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
44194850 19127 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290601 19127 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
44399610 67432 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67432 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11238080 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL205285 75614 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
44424194 85431 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229769 85431 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11504906 75517 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL204881 75517 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279489 123063 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123063 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
4033 1868 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
9826520 1868 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
CHEMBL214957 1868 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
25206454 19063 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290261 19063 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
11671178 76203 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206248 76203 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
16756074 92183 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
CHEMBL243578 92183 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
66873578 127629 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 127629 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
58092270 129250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675278 129250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
12020149 194819 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563412 194819 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455417 97012 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 97012 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
44425807 142882 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389808 142882 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425817 142889 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389810 142889 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424168 85505 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229983 85505 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424172 165619 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL426364 165619 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44389392 122568 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360977 122568 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
11238695 67254 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL190219 67254 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
10210351 122436 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360732 122436 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11317824 81131 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216068 81131 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44415525 80700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 80700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425793 86252 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL231651 86252 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
16756519 92583 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL244163 92583 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
44424072 85197 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85197 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44416650 80264 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215131 80264 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
10239389 126988 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL366161 126988 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
44437555 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44437555 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 168689 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44417880 141149 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385535 141149 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
23567391 62942 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179203 62942 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
45270386 193751 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552229 193751 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
15983865 93499 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
CHEMBL248267 93499 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
20877140 94138 6 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
CHEMBL251948 94138 6 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
49870326 127598 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665365 127598 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
67970575 125886 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651083 125886 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
49868916 129266 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675292 129266 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
58092271 129289 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675314 129289 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
50902096 124102 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640809 124102 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
16043220 77697 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL209964 77697 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416714 140922 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 140922 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11612491 139340 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379927 139340 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
70695565 77635 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL2096889 77635 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430487 86287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL231816 86287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44415525 80700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 80700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424249 85340 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229229 85340 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424232 85491 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229926 85491 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279488 123057 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123057 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL4115701 211140 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
11169159 96347 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL264906 96347 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415526 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425818 160716 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412006 160716 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425790 141733 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL388491 141733 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44424236 85503 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL229980 85503 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
44437528 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437528 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 145673 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437524 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
44437524 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 145669 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
10239389 68988 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL192923 68988 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
11511638 76412 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL206813 76412 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
66873837 127605 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665372 127605 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870049 127640 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665406 127640 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
49868918 129276 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675301 129276 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
44415526 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
10392311 141234 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL386041 141234 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44415526 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 80679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415491 80699 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215621 80699 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424183 85384 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229610 85384 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10238912 75627 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75627 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389490 130148 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL368249 130148 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
25057124 18894 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289053 18894 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
50903069 131310 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693996 131310 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
15983730 168563 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL440229 168563 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44424176 193126 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL538652 193126 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44388077 165809 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
CHEMBL427484 165809 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
49868665 129139 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673558 129139 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
57524844 125890 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651087 125890 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
44417871 165386 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL425084 165386 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
10257298 141012 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384738 141012 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424178 165620 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL426366 165620 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
45279319 122816 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 122816 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25205320 19034 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290042 19034 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
16756637 92771 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 92771 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
44415402 141092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425812 160715 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412005 160715 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417849 96154 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL263296 96154 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
11282697 66927 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL188088 66927 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
45268694 194468 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
CHEMBL561148 194468 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
58580251 125897 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651707 125897 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
49870578 127617 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665384 127617 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
49869913 127588 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665356 127588 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
49869187 129277 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675302 129277 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49869189 129279 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675304 129279 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44414342 77682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 77682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414356 168352 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438615 168352 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44416261 79582 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212756 79582 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10099409 80714 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215666 80714 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10348749 96000 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL262175 96000 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415402 141092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
25205153 19007 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
CHEMBL1289824 19007 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
9848699 60314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176024 60314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
25056872 19011 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289834 19011 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
50903150 131304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693990 131304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
23567276 62851 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL178998 62851 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
44388355 62647 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178546 62647 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397312 67142 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189282 67142 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
49869074 127559 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665327 127559 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
49868799 129145 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673564 129145 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
57524674 125881 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651078 125881 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
50901933 131311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3694003 131311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44417869 80110 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214817 80110 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44424071 141565 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 141565 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
44414444 138078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL377570 138078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44454966 154887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 154887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44416753 140905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 140905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
10053890 79518 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212508 79518 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425798 153216 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398186 153216 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
17989409 79710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL213255 79710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
52948835 18961 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289511 18961 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25205316 19122 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290594 19122 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44416753 140905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 140905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416388 79401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212032 79401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416586 79964 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
CHEMBL214417 79964 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
21101402 140969 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL384489 140969 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
58092218 131309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693995 131309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
11410430 141283 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386311 141283 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415460 137613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 137613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44388265 122350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL360567 122350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44437557 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44437557 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91319 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44416472 80007 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214577 80007 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416428 80909 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL215898 80909 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
44416480 141245 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
CHEMBL386111 141245 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
44416816 79982 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
CHEMBL214504 79982 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
44416522 140867 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL383972 140867 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
44437525 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437525 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 90999 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437520 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437520 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
45272942 194008 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556661 194008 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49869776 123908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3639642 123908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
66874746 127630 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
CHEMBL3665397 127630 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
49868784 129287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675312 129287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
58092286 129893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680175 129893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
50902098 124106 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640815 124106 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
44430489 152323 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL397421 152323 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
10436663 165455 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425434 165455 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
44415460 137613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 137613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424233 85502 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229979 85502 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45278977 123065 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123065 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205321 19145 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290713 19145 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
10230235 131300 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL369392 131300 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44415462 79611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 79611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44440586 150296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL395699 150296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44417989 165618 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL426339 165618 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
10054046 16881 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254711 16881 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437498 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
12020169 193132 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
CHEMBL538711 193132 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
44437498 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147016 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870185 127594 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665361 127594 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
50902097 124103 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3640812 124103 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44417828 80269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
11376122 81475 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216471 81475 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415462 79611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 79611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424199 85449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229875 85449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11635674 200164 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200164 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756753 91696 0 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 91696 0 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
25206134 18890 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289044 18890 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
25205150 19018 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289940 19018 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 90771 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
50902099 124109 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640818 124109 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL4115716 211155 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414466 136951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL375386 136951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44414483 79323 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79323 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430499 86791 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232834 86791 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415446 160820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 160820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
45279319 122816 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 122816 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25017300 19091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290384 19091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16756186 92740 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 92740 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756521 92743 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244373 92743 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
44415446 160820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 160820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
44417863 79879 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214019 79879 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44415440 141221 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141221 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425826 153213 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL398184 153213 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567290 63144 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179872 63144 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
20779442 62945 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179216 62945 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417831 80056 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
CHEMBL214670 80056 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
49868667 129142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673561 129142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
49870577 127616 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665383 127616 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
9799726 141342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386660 141342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414481 138371 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138371 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10256914 79763 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213491 79763 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415440 141221 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141221 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424207 85506 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229986 85506 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692643 76198 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206195 76198 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
16755968 92060 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92060 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
1725351 125898 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
CHEMBL3651708 125898 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
49869629 127576 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665344 127576 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
44425823 142892 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389812 142892 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44539369 148823 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL3945242 148823 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
44424237 141973 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389059 141973 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16072132 80017 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80017 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
25110804 95046 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95046 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44417024 79979 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 79979 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414309 138360 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138360 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430475 86642 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 86642 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430463 148867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 148867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
44397254 66964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL188330 66964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44397095 67208 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL189756 67208 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
44397018 123390 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL362790 123390 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397086 123752 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL363470 123752 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44396800 126288 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL365443 126288 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
16756073 91856 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 91856 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10310772 67435 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
CHEMBL190875 67435 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
44399610 67432 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67432 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11752750 60396 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60396 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911310 125900 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
CHEMBL3651710 125900 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
11340348 128938 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367156 128938 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414399 80511 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL215338 80511 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11511147 165642 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL426507 165642 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44388409 165686 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 165686 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
45279868 123074 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123074 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
25054013 18912 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289169 18912 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
11532924 137854 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 137854 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
11547011 141082 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141082 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
44424258 85347 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229291 85347 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11518999 140375 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382177 140375 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81154 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10203421 67120 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189147 67120 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
45279061 123075 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123075 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
25205319 19048 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290150 19048 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11548597 75872 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205838 75872 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279489 123063 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123063 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194749 19066 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290265 19066 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
44416895 80190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
46187172 121191 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3588863 121191 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
45279061 123075 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123075 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
52942456 19050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
CHEMBL1290155 19050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
16756187 92741 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 92741 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
16006978 79663 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79663 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
71450863 78208 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL2112322 78208 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
25206612 19086 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290378 19086 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
16046124 80050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416895 80190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416757 80737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 80737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
67970248 125887 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651084 125887 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL4115762 211178 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
45266979 193182 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539737 193182 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424261 143482 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL390288 143482 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
11526592 74681 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL203445 74681 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
25057913 18996 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289726 18996 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
20779426 60225 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
CHEMBL175874 60225 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
44425800 148794 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL394502 148794 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567408 167663 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL433608 167663 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
11330800 81862 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217132 81862 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388451 63167 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179974 63167 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11664134 81813 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217080 81813 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11519652 82057 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217618 82057 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
14514271 80071 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214684 80071 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
49870554 129247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675275 129247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
49869188 129278 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675303 129278 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
58092278 129894 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680176 129894 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
44455443 95267 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95267 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416629 80505 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL215321 80505 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44388425 62687 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178755 62687 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44424247 85333 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229178 85333 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424268 143486 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL390290 143486 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389406 62187 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178195 62187 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756522 92744 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL244374 92744 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
44416990 80552 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80552 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
17989409 79710 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213255 79710 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44416479 80081 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
CHEMBL214715 80081 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
16110074 80169 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL214968 80169 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
17989406 81891 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217210 81891 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
18672590 141094 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385254 141094 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416627 79833 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL213817 79833 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44416738 80156 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL214916 80156 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44396904 66545 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL186338 66545 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
11385742 84649 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
CHEMBL224438 84649 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
45270393 193931 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL555875 193931 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424228 85446 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229870 85446 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44437516 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437516 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 90770 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44425806 96576 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266739 96576 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424266 85361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229407 85361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
44416798 80162 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL214941 80162 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
17989383 82054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217610 82054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44417859 80101 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214778 80101 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416990 80552 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80552 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44397200 67035 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188659 67035 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11296279 80139 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214858 80139 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11410080 80724 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL215695 80724 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
49870580 127619 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665386 127619 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
57524585 125875 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651072 125875 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
66603270 129892 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680174 129892 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
44415459 78327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
11698964 75972 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205874 75972 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
25054551 18981 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289624 18981 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
44415459 78327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44415425 140924 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 140924 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44425804 85759 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231216 85759 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44397168 167713 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL433961 167713 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
57524843 125889 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651086 125889 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
46878210 200163 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607120 200163 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
49870811 129271 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675297 129271 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
9985881 79637 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212955 79637 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388365 62755 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178864 62755 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415425 140924 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 140924 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44424198 85442 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229824 85442 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424204 85493 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229930 85493 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
16756184 91707 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 91707 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
44425794 86253 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231652 86253 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425799 153217 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398187 153217 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
11698729 81129 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216066 81129 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397243 123859 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL363876 123859 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
15983733 93369 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247566 93369 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
2729502 80640 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 80640 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
45267015 193107 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL538215 193107 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416364 140913 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384172 140913 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10029835 141218 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385947 141218 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16756751 92878 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 92878 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
173712 123802 19 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL363548 123802 19 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
16756401 150409 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150409 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
52947025 16893 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254796 16893 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44416628 82069 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL217699 82069 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
45268725 194439 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
CHEMBL560953 194439 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
15983862 93412 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247764 93412 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44417839 161111 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL413051 161111 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
10325994 80667 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215501 80667 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
11353108 141581 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL388298 141581 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
16756403 150410 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150410 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
44416781 80025 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80025 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44440592 93263 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246992 93263 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
45272944 194023 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556868 194023 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
58092298 129890 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680172 129890 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
44397163 124533 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364414 124533 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10456385 91708 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 91708 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
10142464 128284 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL366934 128284 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
52941526 18948 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289400 18948 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44424169 142497 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL389483 142497 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424068 85323 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229092 85323 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
11786179 66505 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL186156 66505 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
50902182 124104 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640813 124104 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
11756387 141089 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385218 141089 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10098577 141364 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386819 141364 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415439 81040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
1314 3670 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
9865843 3670 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
CHEMBL178707 3670 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
25017297 19108 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290492 19108 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44415439 81040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11698276 82015 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217430 82015 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437547 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437547 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91315 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
20779429 60221 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175860 60221 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
50903068 131308 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131308 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44430486 86286 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL231815 86286 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415401 79852 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 79852 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16116777 65792 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL184037 65792 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416498 79734 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213370 79734 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416539 79824 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213767 79824 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
21101400 79890 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214081 79890 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416521 140866 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL383971 140866 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
11318577 67683 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
CHEMBL191388 67683 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
11678666 76356 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206498 76356 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
44415396 79756 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 79756 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
10160079 79692 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213171 79692 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
10277257 79991 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214527 79991 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989325 80432 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215257 80432 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416402 138042 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL377541 138042 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416781 80025 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80025 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44415466 139632 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 139632 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
9978490 121908 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 121908 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44417887 140952 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL384400 140952 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44424066 141542 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387990 141542 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
16046124 80050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416757 80737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 80737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430471 86378 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86378 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430459 86736 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 86736 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
44430468 91929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 91929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
44397245 67194 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189650 67194 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397293 123549 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363238 123549 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006978 79663 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79663 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11706744 75189 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204407 75189 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
44417965 81735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216820 81735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
11376081 67690 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL191409 67690 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
11752750 60396 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60396 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911363 125902 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651712 125902 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
44414432 77584 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77584 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424206 167837 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL434747 167837 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10195637 76358 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206503 76358 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44424269 85368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229461 85368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44194954 19106 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290490 19106 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25017571 19128 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290602 19128 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44193792 19148 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290719 19148 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
56673836 65144 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
CHEMBL1830047 65144 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
10140707 63013 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179425 63013 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414318 80153 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214907 80153 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11684498 77298 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208845 77298 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424216 168762 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL441726 168762 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11678040 75108 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204212 75108 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279493 123062 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123062 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
44424193 141537 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387962 141537 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44194849 19065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290264 19065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
49836013 127602 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665369 127602 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
49868670 127560 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665328 127560 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
49869209 127562 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665330 127562 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
57383959 125877 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651074 125877 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
44414571 79865 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 79865 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279583 123073 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123073 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
25057388 18928 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289282 18928 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
25054288 18963 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289515 18963 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
11236807 81154 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81154 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10184368 62970 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179326 62970 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414375 79694 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213187 79694 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
45279583 123073 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123073 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
49869350 127571 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
CHEMBL3665339 127571 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
11454965 82102 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217761 82102 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11455871 141231 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL386035 141231 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44416405 140916 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 140916 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44481638 65148 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830051 65148 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
44462720 65149 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830052 65149 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
50908737 18945 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 18945 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44417840 81476 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
CHEMBL216472 81476 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
10304239 194153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL558277 194153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44415401 79852 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 79852 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425797 165776 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL427262 165776 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44415396 79756 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 79756 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415466 139632 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 139632 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11410594 96753 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL268385 96753 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416140 79383 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211964 79383 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415414 138151 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138151 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
45272984 194043 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL557070 194043 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416391 81121 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL216038 81121 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44440589 148560 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394310 148560 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44424067 142655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 142655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44415414 138151 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138151 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
49869211 127564 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665332 127564 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
44437522 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437522 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 90808 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437496 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437496 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91558 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44414552 79645 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL212979 79645 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416322 80093 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214750 80093 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44388311 62692 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178772 62692 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
16745305 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
16756524 143388 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL390212 143388 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
25057645 18997 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289727 18997 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
44415431 79655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 79655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
16745305 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 145847 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44388309 122771 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361423 122771 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
49870700 129138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673557 129138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
49870325 127597 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665364 127597 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
66873755 127652 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665418 127652 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
44425803 96575 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266738 96575 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415431 79655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 79655 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
44417868 80444 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215273 80444 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
58092274 129249 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675277 129249 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
9984325 96242 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL263975 96242 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430501 150656 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395979 150656 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44425837 85603 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230626 85603 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44416346 79448 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212230 79448 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389546 64442 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181931 64442 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45267814 194428 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560888 194428 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
44414601 138407 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL378439 138407 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44430488 86326 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232027 86326 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44416178 139364 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379940 139364 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424252 137042 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL375466 137042 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10229815 62007 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177900 62007 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL4115703 211142 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44389604 63961 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
CHEMBL181020 63961 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
45272117 193591 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL551149 193591 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49869774 127583 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
CHEMBL3665351 127583 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
57524506 125870 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
CHEMBL3651067 125870 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
58092289 129253 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
CHEMBL3675280 129253 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
66603252 129292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675317 129292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
44455367 95185 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95185 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
16755967 92138 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243354 92138 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44415463 79612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 79612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 79599 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 79599 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415463 79612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 79612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424205 85494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229931 85494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424173 142498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
CHEMBL389484 142498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
44389354 63605 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180658 63605 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
25017299 19129 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
CHEMBL1290603 19129 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
44415516 138762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 138762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 79599 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 79599 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870679 129248 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675276 129248 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44417852 141127 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385393 141127 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
49868939 127550 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3665318 127550 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL4115761 211177 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44430484 86285 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL231814 86285 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415516 138762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 138762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16756404 92434 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244003 92434 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49869348 127568 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665336 127568 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49869349 127569 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665337 127569 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49870453 127601 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665368 127601 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
45270392 193366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL549395 193366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455414 96968 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 96968 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416801 79897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 79897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 96686 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 96686 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430455 86424 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86424 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430483 87945 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234931 87945 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44397497 66951 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL188206 66951 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
44397273 67128 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189190 67128 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44424187 85421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229715 85421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
25205318 19033 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290041 19033 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10137322 148876 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 148876 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44416801 79897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 79897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 96686 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 96686 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416405 140916 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 140916 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416390 141145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44455444 94602 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 94602 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
11610423 165466 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 165466 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
44388227 60475 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL176142 60475 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
56660001 65143 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830046 65143 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424210 85325 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229112 85325 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
52941699 18946 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289396 18946 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25017033 19090 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19090 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
49869346 127566 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665334 127566 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
50903153 124100 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124100 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44389379 64303 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181776 64303 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279773 123068 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123068 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756642 92847 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 92847 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44414576 79628 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL212922 79628 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44414589 79754 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 79754 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424231 85490 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229925 85490 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
10186375 78538 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL2112988 78538 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
10141528 122435 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL360731 122435 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44388428 62977 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179346 62977 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
1314 3670 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
9865843 3670 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
CHEMBL178707 3670 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
45279773 123068 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123068 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
11329623 81683 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216570 81683 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
52942796 18979 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289620 18979 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
11752320 67390 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL190780 67390 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
10206922 130182 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL368417 130182 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416390 141145 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141145 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44424189 141536 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387961 141536 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
49869491 127574 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665342 127574 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
25205829 19049 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290151 19049 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11420621 66840 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL187721 66840 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
49870699 129137 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673556 129137 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
66873929 127651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665417 127651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
44388417 62892 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179072 62892 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11785261 67243 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67243 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
44430465 92867 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 92867 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
44425789 85522 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230080 85522 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16755872 92064 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92064 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
10185187 62969 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179325 62969 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44416553 79513 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
CHEMBL212487 79513 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
44416503 79978 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
CHEMBL214494 79978 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
17989373 80435 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215261 80435 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416606 80665 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215493 80665 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
44416502 168397 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
CHEMBL438966 168397 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
44416880 82037 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82037 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44427407 141569 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
CHEMBL388234 141569 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
46911144 125899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651709 125899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
11273638 84725 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
CHEMBL225073 84725 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
44416880 82037 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82037 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416580 141405 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL387081 141405 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
44416623 80010 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214584 80010 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44417878 140851 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383859 140851 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437519 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
12020152 193782 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552432 193782 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
16046157 140980 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384548 140980 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
44415427 79629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 79629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 139525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 139525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
44424265 143485 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
CHEMBL390289 143485 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
44415427 79629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 79629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 139525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 139525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
11342100 84681 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224686 84681 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
10483729 16769 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253625 16769 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45269555 194445 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561011 194445 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44437519 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 90807 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44388314 130145 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL368228 130145 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
58093407 127620 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665387 127620 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
44415410 77580 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77580 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424184 85395 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229665 85395 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44415410 77580 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77580 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415426 141307 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141307 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424175 85378 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229557 85378 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
25205493 18992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289718 18992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
10348147 79755 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213464 79755 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415426 141307 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141307 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424170 85373 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229504 85373 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424250 85504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229981 85504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
45278576 123069 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123069 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756523 92769 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244576 92769 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
44437494 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437494 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91467 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424238 85329 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229164 85329 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44417829 80177 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215004 80177 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414506 141320 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386512 141320 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45268721 195064 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL565119 195064 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49870327 127599 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665366 127599 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414461 79840 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL213840 79840 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424270 85370 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229463 85370 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389509 62343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178388 62343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44417984 141292 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386354 141292 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
57524672 125879 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
CHEMBL3651076 125879 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
44437499 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437499 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91560 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870807 129256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675283 129256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
50902014 124099 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
CHEMBL3640806 124099 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
10029161 141359 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386759 141359 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
25018073 19150 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290721 19150 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44437523 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
44437523 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 145668 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
49868806 127546 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665314 127546 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870050 127641 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665407 127641 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
49836011 129268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675294 129268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
44416862 80654 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 80654 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430453 87494 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87494 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
44425835 85589 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230521 85589 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425839 150696 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396008 150696 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16006976 82032 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82032 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424191 85429 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229767 85429 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11627700 82044 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217574 82044 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11452967 67189 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189611 67189 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
10140070 67282 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL190401 67282 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
49869212 127565 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665333 127565 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
25017572 19068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290267 19068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11329860 141150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL385539 141150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416862 80654 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 80654 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
49836016 129136 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
CHEMBL3673555 129136 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
49869210 127563 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665331 127563 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
66873757 127628 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665395 127628 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
9895005 138903 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379391 138903 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16006976 82032 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82032 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
50903153 124100 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124100 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44481364 65150 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830053 65150 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
45279064 123078 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123078 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
45279062 123081 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123081 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
45279062 123081 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123081 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11168918 81249 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216368 81249 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
56666883 65140 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830043 65140 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44194853 19089 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290382 19089 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
11191656 140859 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383901 140859 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414654 79926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214254 79926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10077403 138402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL378428 138402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
58093324 127625 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665392 127625 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49869778 127585 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665353 127585 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
49870328 127600 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665367 127600 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49868678 127646 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665412 127646 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
44416607 165385 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165385 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44424197 142531 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL389517 142531 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11192044 77634 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL2096864 77634 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
44397103 123913 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363965 123913 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44437501 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
11641333 168178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
CHEMBL437130 168178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
44437501 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 153899 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44396985 124131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364134 124131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11720881 81466 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216460 81466 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11610423 165466 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165466 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
67970371 125888 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651085 125888 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
57524762 125884 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
CHEMBL3651081 125884 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
44417860 80102 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL214779 80102 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
52942550 19103 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290484 19103 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44425820 96845 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL269061 96845 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44417870 80015 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214606 80015 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
10029836 80698 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215619 80698 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44396975 121740 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL359782 121740 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44416916 80997 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 80997 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416607 165385 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165385 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416561 79739 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213386 79739 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416664 82410 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
CHEMBL218030 82410 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
10295411 165584 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL426147 165584 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
11489282 143597 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL390377 143597 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
44415381 80164 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80164 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415381 80164 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80164 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415407 138910 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 138910 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
52944805 16770 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253626 16770 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437514 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437514 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 89914 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44389526 62919 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL179115 62919 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
44389375 64002 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181176 64002 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44425805 85545 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230307 85545 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415407 138910 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 138910 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11670645 85375 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229512 85375 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417854 80402 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215224 80402 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
16756638 92797 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 92797 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
52948254 16906 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254883 16906 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44417853 81127 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216056 81127 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44389378 63689 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180717 63689 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
50903154 131307 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693993 131307 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44388096 63180 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL180009 63180 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49870579 127618 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665385 127618 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
44416916 80997 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 80997 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430480 87934 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234929 87934 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
58092292 129259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675286 129259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49869327 129281 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675306 129281 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44417850 81245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424070 85324 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85324 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44430477 86790 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 86790 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
10031575 138729 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379002 138729 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430476 151774 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 151774 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397087 66807 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187558 66807 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006977 139633 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 139633 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424180 141472 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL387502 141472 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692133 75079 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204161 75079 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
44194579 18926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289278 18926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
46911147 125901 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651711 125901 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
49868804 127543 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665311 127543 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
57524505 125869 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651066 125869 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
44414540 79916 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 79916 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
10217978 140555 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382631 140555 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
44399507 124650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
CHEMBL364500 124650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
11420203 67572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL191078 67572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
11752579 67573 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL191079 67573 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
122180707 121252 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3589155 121252 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
49869072 127556 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665324 127556 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
49869630 127578 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665346 127578 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
44414391 79787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 79787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424229 85447 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229871 85447 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
16718619 121251 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121251 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
52949941 18911 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289166 18911 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
49870323 127595 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665362 127595 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
49870455 127604 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665371 127604 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44389391 122567 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360976 122567 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
11156521 66892 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL187931 66892 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
49869912 127587 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665355 127587 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
10159789 60241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175943 60241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
16006977 139633 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 139633 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
58093333 127610 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665377 127610 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
16755969 91883 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 91883 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
49870181 127643 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665409 127643 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
44424192 85430 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229768 85430 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52947558 18927 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289279 18927 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
52941539 18962 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289512 18962 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
49869914 127589 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665357 127589 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
66874257 127632 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665399 127632 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
50903065 131303 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131303 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44224161 65141 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830044 65141 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424202 85451 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229877 85451 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52944997 19126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290600 19126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
11785262 69051 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69051 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
45279233 123084 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123084 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11752339 69056 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69056 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
44416989 80501 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80501 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430495 167077 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL430162 167077 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
16756402 92414 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92414 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
11409615 141233 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386039 141233 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
15983864 93498 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL248266 93498 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
52944068 19036 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290046 19036 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
58093391 127649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665415 127649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
57524584 125874 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651071 125874 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
57524587 125878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651075 125878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
44416287 138773 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL379201 138773 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
11577708 75205 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204514 75205 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL4115717 211156 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416311 79662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213050 79662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415467 79670 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 79670 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
49869777 127584 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665352 127584 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
44415467 79670 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 79670 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
50901936 131316 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
CHEMBL3694008 131316 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
44389422 168052 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL436081 168052 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
3575822 153809 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
CHEMBL398687 153809 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
3787955 154085 12 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
CHEMBL399303 154085 12 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
49870682 129258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675285 129258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
45278657 123059 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123059 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44437620 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44416172 77736 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL210167 77736 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44416225 137859 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377251 137859 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416966 140936 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL384302 140936 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
12020156 194608 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL562016 194608 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
44437620 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145156 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
67970689 125876 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651073 125876 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
44414542 79925 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 79925 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
4826270 94136 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
CHEMBL251946 94136 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
16116777 65792 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
CHEMBL184037 65792 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
44416554 79514 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
CHEMBL212488 79514 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
44416584 79859 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213922 79859 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416968 81126 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL216054 81126 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416495 141067 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL385054 141067 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
44416735 141093 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385253 141093 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
10277136 141333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL386600 141333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416841 79895 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214123 79895 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020168 193157 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539227 193157 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416174 141395 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL387025 141395 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416989 80501 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80501 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430494 86582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232439 86582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
16739310 85604 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230627 85604 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44425811 96542 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266513 96542 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415451 79646 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 79646 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11533835 76418 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206831 76418 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279488 123057 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123057 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58092287 129254 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675281 129254 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
44415451 79646 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 79646 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
66873669 127606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665373 127606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
11719877 85369 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229462 85369 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
16756752 142059 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142059 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
11260997 66908 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187996 66908 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
57524676 125883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
CHEMBL3651080 125883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
49869050 129275 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675300 129275 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49868915 129265 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675291 129265 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
11272081 81046 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215964 81046 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11590806 77914 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210926 77914 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
52941621 19008 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289829 19008 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
66898224 127609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665376 127609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49869048 129273 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
CHEMBL3675299 129273 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
49868780 129283 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675308 129283 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
44414649 139428 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379978 139428 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
16755971 92150 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL243507 92150 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
11691555 3729 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
1319 3729 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
CHEMBL384701 3729 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
44417835 81750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216953 81750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414528 138125 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
CHEMBL377664 138125 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
44388442 122606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361139 122606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
58093393 127626 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665393 127626 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424224 85344 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229285 85344 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424208 85507 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229988 85507 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279321 123080 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123080 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58093416 127608 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665375 127608 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414310 137953 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 137953 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
11785262 69051 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69051 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
49869633 127581 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665349 127581 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
66874268 127650 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665416 127650 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
11648753 140210 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL381810 140210 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424259 141868 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL388972 141868 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
11648753 140210 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381810 140210 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
11168186 67686 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 67686 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
11168186 67686 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
CHEMBL191393 67686 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
11489130 167661 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL433596 167661 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
44430479 170294 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL445407 170294 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
44424235 85195 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL228289 85195 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44425822 160717 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412007 160717 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44416689 80844 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215873 80844 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44417872 141254 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386163 141254 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
57524846 125893 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
CHEMBL3651090 125893 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
2276336 167117 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
CHEMBL430208 167117 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
44389405 62696 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178808 62696 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
17989439 93161 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246588 93161 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
10007632 79908 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214185 79908 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389440 62178 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
CHEMBL178147 62178 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
44388201 127297 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL366445 127297 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417061 96584 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL266840 96584 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425830 85602 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230625 85602 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756520 92742 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244372 92742 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44424267 85362 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229408 85362 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417836 82062 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL217653 82062 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
45279491 123058 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123058 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416173 140897 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384116 140897 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
45278657 123059 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123059 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44425802 142642 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389608 142642 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417842 81737 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216828 81737 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44480332 65145 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
CHEMBL1830048 65145 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
11752339 69056 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL193260 69056 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10239907 138206 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL378019 138206 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
45279233 123084 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123084 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
57524673 125880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 125880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
45279872 123079 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123079 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
66873409 127634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665400 127634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
11785261 67243 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67243 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
10297428 61654 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177426 61654 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
57524673 125880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 125880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
50903068 131308 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131308 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL4115702 211141 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
10415704 80734 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215728 80734 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
11613829 76102 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205979 76102 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
49869351 127570 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665338 127570 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
58093338 127611 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665378 127611 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44424209 137063 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL375520 137063 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
25057911 18964 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
CHEMBL1289516 18964 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
49869070 127553 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665321 127553 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
58093402 127647 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665413 127647 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
11511671 140677 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL382841 140677 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45279872 123079 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123079 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
11168186 67686 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 67686 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
66886732 127645 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665411 127645 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
58092272 129255 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675282 129255 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
50901931 131313 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694005 131313 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
11758499 157272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL408332 157272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424234 141972 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL389058 141972 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
24857597 19067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290266 19067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
9985634 79347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870456 127614 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665381 127614 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
50903068 131308 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131308 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
49870048 127639 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665405 127639 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
44424254 85346 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229290 85346 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44397227 66831 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187660 66831 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
44416929 140907 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384156 140907 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
44425824 54531 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL161261 54531 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424200 85450 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229876 85450 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424201 142534 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL389518 142534 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11496824 81174 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216286 81174 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
44416275 80818 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL215850 80818 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44417891 79942 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214323 79942 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44425814 85658 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230940 85658 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
45272985 194044 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557071 194044 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
57524761 125885 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
CHEMBL3651082 125885 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
44437526 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44416223 138730 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379004 138730 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44437526 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 91000 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44389390 62617 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178496 62617 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
11642491 81170 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216267 81170 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437553 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437553 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 90714 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
50902011 131317 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694009 131317 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44409689 76416 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206825 76416 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
44389590 62181 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
CHEMBL178182 62181 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
11306487 66839 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
CHEMBL187719 66839 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
11202371 84656 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224519 84656 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
11192042 136825 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL375291 136825 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
50902015 124107 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640816 124107 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
44418000 141402 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL387065 141402 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
25206298 19087 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290379 19087 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
11520239 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3575 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1311 3391 0 None - 1 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
1295 3387 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
155817404 3387 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1298 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16167454 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16167454 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
91898993 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
91898993 2449 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1294 3386 0 None -1 2 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1294 3386 0 None 1 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1302 3912 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
155817405 3912 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1295 3387 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
155817404 3387 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1309 3389 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1308 3388 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1312 3471 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
16046160 3471 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
11238212 507 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1304 507 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1310 3390 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1291 753 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
268 753 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
11691555 3729 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1319 3729 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
CHEMBL384701 3729 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1297 3054 0 None - 1 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101600353 2435 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1301 2435 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
134824567 2435 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16207764 2435 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101110542 2436 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1293 2436 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101600353 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
101600353 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1301 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1301 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
134824567 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
134824567 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16207764 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16207764 2435 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101110542 2436 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1293 2436 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2449 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16167454 2449 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
91898993 2449 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073