Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44417940 81725 None 0 Human Functional pEC50 = 6 6.0 - 1
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 81725 None 0 Human Functional pEC50 = 6 6.0 - 1
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 158541 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 158541 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 158541 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 158541 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 81624 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 81624 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 141897 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 141897 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 80615 None 0 Rat Functional pEC50 = 7.0 7.0 -8 2
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 80615 None 0 Rat Functional pEC50 = 7.0 7.0 -8 2
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 81156 None 0 Rat Functional pEC50 = 7.0 7.0 -9 2
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 81156 None 0 Rat Functional pEC50 = 7.0 7.0 -9 2
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 81495 None 0 Rat Functional pEC50 = 7.0 7.0 -10 2
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 81495 None 0 Rat Functional pEC50 = 7.0 7.0 -10 2
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 80825 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 80825 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 165867 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 165867 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 141855 None 0 Rat Functional pEC50 = 5.9 5.9 -67 2
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 141855 None 0 Rat Functional pEC50 = 5.9 5.9 -67 2
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 16706 None 3 Human Functional pEC50 = 6.9 6.9 -13 2
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 16706 None 3 Human Functional pEC50 = 6.9 6.9 -13 2
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 16706 None 3 Human Functional pEC50 = 6.9 6.9 -13 2
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 16706 None 3 Human Functional pEC50 = 6.9 6.9 -13 2
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 208808 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 208808 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 81150 None 0 Rat Functional pEC50 = 6.9 6.9 -70 2
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 81150 None 0 Rat Functional pEC50 = 6.9 6.9 -70 2
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 82474 None 0 Rat Functional pEC50 = 6.9 6.9 -281 2
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 82474 None 0 Rat Functional pEC50 = 6.9 6.9 -281 2
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 141647 None 0 Rat Functional pEC50 = 6.9 6.9 -14 2
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 141647 None 0 Rat Functional pEC50 = 6.9 6.9 -14 2
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 82427 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82427 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82240 None 0 Rat Functional pEC50 = 6.8 6.8 -151 2
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 82240 None 0 Rat Functional pEC50 = 6.8 6.8 -151 2
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 82117 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82117 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82130 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82130 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 95543 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 95543 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 155516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 155516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 82127 None 0 Rat Functional pEC50 = 5.8 5.8 -70 2
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 82127 None 0 Rat Functional pEC50 = 5.8 5.8 -70 2
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 81894 None 0 Rat Functional pEC50 = 5.8 5.8 -48 2
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 81894 None 0 Rat Functional pEC50 = 5.8 5.8 -48 2
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 82332 None 0 Rat Functional pEC50 = 6.7 6.7 -63 2
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 82332 None 0 Rat Functional pEC50 = 6.7 6.7 -63 2
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 95098 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 95098 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97471 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97471 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 91549 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 91549 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 91559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 91559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 141600 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 141600 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 141781 None 0 Rat Functional pEC50 = 6.7 6.7 -16 2
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 141781 None 0 Rat Functional pEC50 = 6.7 6.7 -16 2
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 141634 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 141634 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 91556 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 91556 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 96704 None 0 Rat Functional pEC50 = 7.6 7.6 -3 2
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 96704 None 0 Rat Functional pEC50 = 7.6 7.6 -3 2
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 141598 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 141598 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 81151 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 81151 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 91561 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 91561 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 82470 None 0 Human Functional pEC50 = 6.6 6.6 13 2
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 82470 None 0 Human Functional pEC50 = 6.6 6.6 13 2
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 80337 None 0 Rat Functional pEC50 = 6.6 6.6 -53 2
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 80337 None 0 Rat Functional pEC50 = 6.6 6.6 -53 2
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 81992 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 81992 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 141785 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 141785 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 169122 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 169122 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 95683 None 0 Human Functional pEC50 = 7.5 7.5 831 2
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 95683 None 0 Human Functional pEC50 = 7.5 7.5 831 2
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 91551 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91551 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91553 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91553 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91557 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91557 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91558 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 91558 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 141795 None 0 Rat Functional pEC50 = 7.5 7.5 -5 2
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 141795 None 0 Rat Functional pEC50 = 7.5 7.5 -5 2
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 82489 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 82489 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 80876 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 80876 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 141743 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 141743 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 80950 None 0 Rat Functional pEC50 = 6.5 6.5 -104 2
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 80950 None 0 Rat Functional pEC50 = 6.5 6.5 -104 2
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 80436 None 0 Rat Functional pEC50 = 6.5 6.5 -16 2
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 80436 None 0 Rat Functional pEC50 = 6.5 6.5 -16 2
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 82237 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 82237 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 80638 None 0 Rat Functional pEC50 = 6.5 6.5 -173 2
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 80638 None 0 Rat Functional pEC50 = 6.5 6.5 -173 2
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 82473 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 82473 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 82467 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 82467 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 80590 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 80590 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 81588 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 81588 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 95764 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 95764 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 91552 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 91552 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 141973 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 141973 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 141810 None 0 Rat Functional pEC50 = 6.4 6.4 -199 2
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 141810 None 0 Rat Functional pEC50 = 6.4 6.4 -199 2
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 161612 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 161612 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 80946 None 0 Rat Functional pEC50 = 6.4 6.4 -87 2
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 80946 None 0 Rat Functional pEC50 = 6.4 6.4 -87 2
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 91555 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 91555 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 141947 None 0 Rat Functional pEC50 = 6.3 6.3 -2 2
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 141947 None 0 Rat Functional pEC50 = 6.3 6.3 -2 2
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 141884 None 0 Rat Functional pEC50 = 7.3 7.3 -16 2
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 141884 None 0 Rat Functional pEC50 = 7.3 7.3 -16 2
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 81628 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 81628 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 81168 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 81168 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 91560 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 91560 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 82471 None 0 Rat Functional pEC50 = 7.3 7.3 -14 2
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 82471 None 0 Rat Functional pEC50 = 7.3 7.3 -14 2
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 141476 None 0 Rat Functional pEC50 = 6.2 6.2 1 2
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 141476 None 0 Rat Functional pEC50 = 6.2 6.2 1 2
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 91554 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 91554 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141973 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141973 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141973 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141973 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 80321 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 80321 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 82177 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 82177 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 141836 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141836 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 95682 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 95682 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 91547 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 91547 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141562 None 0 Rat Functional pEC50 = 7.2 7.2 -5 2
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 141562 None 0 Rat Functional pEC50 = 7.2 7.2 -5 2
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 141674 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141674 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141748 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 141748 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 82544 None 0 Rat Functional pEC50 = 6.1 6.1 -3 2
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 82544 None 0 Rat Functional pEC50 = 6.1 6.1 -3 2
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 141709 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 141709 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 141839 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 141839 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 166037 None 0 Rat Functional pEC50 = 6.1 6.1 -9 2
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 166037 None 0 Rat Functional pEC50 = 6.1 6.1 -9 2
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 81826 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 81826 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 141757 None 0 Rat Functional pEC50 = 7.1 7.1 -89 2
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 141757 None 0 Rat Functional pEC50 = 7.1 7.1 -89 2
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 82500 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 82500 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 81490 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 81490 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 82597 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 82597 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 80616 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 80616 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 141904 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 141904 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 80871 None 0 Human Functional pEC50 = 6 6.0 - 1
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 80871 None 0 Human Functional pEC50 = 6 6.0 - 1
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 1004 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 1004 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 1004 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 1899 None 38 Human Functional pIC50 = 9.3 9.3 - 1
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 74978 None 7 Mouse Functional pIC50 = 9.2 9.2 1 5
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 74978 None 7 Mouse Functional pIC50 = 9.2 9.2 1 5
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 82430 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 82430 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 82923 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 82923 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 74978 None 7 Rat Functional pIC50 = 9.1 9.1 -1 5
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 74978 None 7 Rat Functional pIC50 = 9.1 9.1 -1 5
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 74978 None 7 Rhesus macaque Functional pIC50 = 9.1 9.1 -1 5
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 74978 None 7 Rhesus macaque Functional pIC50 = 9.1 9.1 -1 5
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 141798 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 141798 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 141910 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 141910 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 141521 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 141521 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 80848 None 0 Human Functional pIC50 = 9 9.0 - 1
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 80848 None 0 Human Functional pIC50 = 9 9.0 - 1
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 80094 None 0 Human Functional pIC50 = 9 9.0 - 1
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 80094 None 0 Human Functional pIC50 = 9 9.0 - 1
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 94355 None 0 Human Functional pIC50 = 9 9.0 - 1
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 94355 None 0 Human Functional pIC50 = 9 9.0 - 1
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 80551 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 80551 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 82324 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 82324 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 82624 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 82624 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 74978 None 7 Human Functional pIC50 = 8.9 8.9 -1 5
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 74978 None 7 Human Functional pIC50 = 8.9 8.9 -1 5
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 79996 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 79996 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 80585 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 80585 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 81582 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 81582 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 82595 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 82595 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 82542 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 82542 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 80606 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 80606 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 80273 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 80273 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 81148 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 81148 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 169389 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 169389 None 0 Human Functional pIC50 = 8.8 8.8 - 1
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 141627 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 141627 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 80369 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 80369 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 78104 None 0 Human Functional pIC50 = 8 8.0 - 1
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 78104 None 0 Human Functional pIC50 = 8 8.0 - 1
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 80264 None 0 Human Functional pIC50 = 8 8.0 - 1
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 80264 None 0 Human Functional pIC50 = 8 8.0 - 1
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 81507 None 0 Human Functional pIC50 = 8 8.0 - 1
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 81507 None 0 Human Functional pIC50 = 8 8.0 - 1
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 200976 None 0 Human Functional pIC50 = 8 8.0 30 4
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 200976 None 0 Human Functional pIC50 = 8 8.0 30 4
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 86840 None 0 Human Functional pIC50 = 8 8.0 - 1
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 86840 None 0 Human Functional pIC50 = 8 8.0 - 1
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 87260 None 0 Human Functional pIC50 = 8 8.0 - 1
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 87260 None 0 Human Functional pIC50 = 8 8.0 - 1
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 149487 None 1 Human Functional pIC50 = 8 8.0 - 1
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 149487 None 1 Human Functional pIC50 = 8 8.0 - 1
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 74869 None 0 Human Functional pIC50 = 8 8.0 1 2
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 74869 None 0 Human Functional pIC50 = 8 8.0 1 2
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 74914 None 0 Human Functional pIC50 = 8 8.0 2 2
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 74914 None 0 Human Functional pIC50 = 8 8.0 2 2
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 124335 None 0 Human Functional pIC50 = 8 8.0 - 1
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 124335 None 0 Human Functional pIC50 = 8 8.0 - 1
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 65605 None 0 Human Functional pIC50 = 8 8.0 - 1
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 65605 None 0 Human Functional pIC50 = 8 8.0 - 1
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 82151 None 0 Human Functional pIC50 = 7 7.0 - 1
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 82151 None 0 Human Functional pIC50 = 7 7.0 - 1
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 142038 None 0 Human Functional pIC50 = 7 7.0 - 1
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 142038 None 0 Human Functional pIC50 = 7 7.0 - 1
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 200949 None 0 Human Functional pIC50 = 7 7.0 - 1
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 200949 None 0 Human Functional pIC50 = 7 7.0 - 1
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 60605 None 0 Human Functional pIC50 = 7 7.0 - 1
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 60605 None 0 Human Functional pIC50 = 7 7.0 - 1
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 199088 None 0 Human Functional pIC50 = 7 7.0 - 1
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 199088 None 0 Human Functional pIC50 = 7 7.0 - 1
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 73535 None 0 Human Functional pIC50 = 7 7.0 - 1
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 73535 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68866 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68866 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68868 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68868 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68878 None 0 Human Functional pIC50 = 7 7.0 - 1
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 68878 None 0 Human Functional pIC50 = 7 7.0 - 1
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 122422 None 0 Human Functional pIC50 = 7 7.0 - 1
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 122422 None 0 Human Functional pIC50 = 7 7.0 - 1
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 123698 None 0 Human Functional pIC50 = 7 7.0 - 1
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 123698 None 0 Human Functional pIC50 = 7 7.0 - 1
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 131520 None 0 Human Functional pIC50 = 7 7.0 - 1
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 131520 None 0 Human Functional pIC50 = 7 7.0 - 1
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 165872 None 0 Human Functional pIC50 = 7 7.0 - 1
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 165872 None 0 Human Functional pIC50 = 7 7.0 - 1
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 76887 None 0 Human Functional pIC50 = 7 7.0 - 1
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 76887 None 0 Human Functional pIC50 = 7 7.0 - 1
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 198595 None 0 Human Functional pIC50 = 6 6.0 - 1
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 198595 None 0 Human Functional pIC50 = 6 6.0 - 1
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 139213 None 0 Human Functional pIC50 = 6 6.0 - 1
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 139213 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68864 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68864 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68867 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68867 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68880 None 0 Human Functional pIC50 = 6 6.0 - 1
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 68880 None 0 Human Functional pIC50 = 6 6.0 - 1
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 82442 None 0 Human Functional pIC50 = 6 6.0 - 1
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 82442 None 0 Human Functional pIC50 = 6 6.0 - 1
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 82494 None 0 Human Functional pIC50 = 7 7.0 - 1
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 82494 None 0 Human Functional pIC50 = 7 7.0 - 1
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 80498 None 0 Human Functional pIC50 = 7 7.0 - 1
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 80498 None 0 Human Functional pIC50 = 7 7.0 - 1
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 37780 None 24 Human Functional pIC50 = 5 5.0 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 37780 None 24 Human Functional pIC50 = 5 5.0 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60604 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 60604 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 189327 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 189327 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 82191 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 82191 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 73491 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 73491 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 72154 None 5 Human Functional pIC50 = 6.0 6.0 - 1
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 72154 None 5 Human Functional pIC50 = 6.0 6.0 - 1
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 177069 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 177069 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 78137 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 78137 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 179097 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 179097 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 125944 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 125944 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 32630 None 5 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 32630 None 5 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 59171 None 0 Human Functional pIC50 = 5.0 5.0 -15 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59171 None 0 Human Functional pIC50 = 5.0 5.0 -15 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59226 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59226 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 35310 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 35310 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 16252 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16252 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 71874 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 71874 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 73579 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73579 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 199193 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 199193 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 80526 None 0 Human Functional pIC50 = 7.0 7.0 11 2
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 80526 None 0 Human Functional pIC50 = 7.0 7.0 11 2
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 70539 None 0 Human Functional pIC50 = 7.0 7.0 173 2
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 70539 None 0 Human Functional pIC50 = 7.0 7.0 173 2
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 60652 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 60652 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 87252 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 87252 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 152395 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 152395 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 74919 None 0 Human Functional pIC50 = 8.0 8.0 162 2
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 74919 None 0 Human Functional pIC50 = 8.0 8.0 162 2
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 56725 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 56725 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 68102 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 68102 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 68107 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 68107 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 64753 None 0 Rat Functional pIC50 = 8.0 8.0 -12 3
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 64753 None 0 Rat Functional pIC50 = 8.0 8.0 -12 3
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 71487 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 71487 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 63380 None 0 Human Functional pIC50 = 8.0 8.0 -2 2
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 63380 None 0 Human Functional pIC50 = 8.0 8.0 -2 2
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 71956 None 0 Human Functional pIC50 = 8.0 8.0 588 2
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 71956 None 0 Human Functional pIC50 = 8.0 8.0 588 2
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 73172 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73172 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16049 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16049 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16067 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16067 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 93365 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 93365 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 67055 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 67055 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 66155 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 66155 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 59743 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59743 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59356 None 0 Human Functional pIC50 = 5.0 5.0 -10 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59356 None 0 Human Functional pIC50 = 5.0 5.0 -10 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 125933 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 125933 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 59884 None 0 Human Functional pIC50 = 5.0 5.0 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59884 None 0 Human Functional pIC50 = 5.0 5.0 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 23337 None 0 Human Functional pIC50 = 5.0 5.0 -1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23337 None 0 Human Functional pIC50 = 5.0 5.0 -1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 21834 None 5 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 21834 None 5 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 16237 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16237 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 82108 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 82108 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 124416 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 124416 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 52309 None 11 Human Functional pIC50 = 5.0 5.0 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 52309 None 11 Human Functional pIC50 = 5.0 5.0 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 60603 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 60603 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 59660 None 0 Human Functional pIC50 = 5.0 5.0 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59660 None 0 Human Functional pIC50 = 5.0 5.0 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 125951 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 125951 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 66239 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 66239 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 96926 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 96926 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 73480 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73480 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125937 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125937 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 71101 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 71101 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 179295 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 179295 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125932 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125932 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 121827 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 121827 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 94059 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 94059 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 42512 None 2 Human Functional pIC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 42512 None 2 Human Functional pIC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80302 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 80302 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 141701 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 141701 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 166114 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 166114 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 60666 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 60666 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 74916 None 0 Human Functional pIC50 = 7.9 7.9 57 2
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 74916 None 0 Human Functional pIC50 = 7.9 7.9 57 2
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 73630 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73630 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 204306 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 204306 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 72336 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 72336 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 80276 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 80276 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 83124 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 83124 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 81266 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 81266 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 80195 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 80195 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 200975 None 0 Human Functional pIC50 = 6.9 6.9 1 5
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 200975 None 0 Human Functional pIC50 = 6.9 6.9 1 5
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 93616 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 93616 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73523 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73523 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 67245 None 0 Mouse Functional pIC50 = 6.9 6.9 -12 2
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 67245 None 0 Mouse Functional pIC50 = 6.9 6.9 -12 2
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 139245 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 139245 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 67102 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 67102 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 59550 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59550 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 26412 None 6 Human Functional pIC50 = 4.9 4.9 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 26412 None 6 Human Functional pIC50 = 4.9 4.9 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 198438 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 198438 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125935 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125935 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 51813 None 5 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51813 None 5 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 198911 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 198911 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 189212 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 189212 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 59610 None 0 Human Functional pIC50 = 4.9 4.9 -8 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59610 None 0 Human Functional pIC50 = 4.9 4.9 -8 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 125930 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125930 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 80406 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 80406 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 59807 None 12 Human Functional pIC50 = 4.9 4.9 -9 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59807 None 12 Human Functional pIC50 = 4.9 4.9 -9 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 46144 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 46144 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55174 None 5 Human Functional pIC50 = 4.9 4.9 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55174 None 5 Human Functional pIC50 = 4.9 4.9 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55174 None 5 Human Functional pIC50 = 4.9 4.9 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 82400 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 82400 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 97031 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 97031 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 65783 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 65783 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 59858 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59858 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 50750 None 1 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 50750 None 1 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 94100 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 94100 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 59834 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59834 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 55284 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55284 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55284 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 201003 None 0 Human Functional pIC50 = 7.9 7.9 9 4
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 201003 None 0 Human Functional pIC50 = 7.9 7.9 9 4
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 142035 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 142035 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 87198 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 87198 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 121830 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 121830 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73627 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73627 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73628 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73628 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 92619 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
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 92619 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
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 138987 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 138987 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 60599 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 60599 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 92174 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 92174 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 67274 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 67274 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 66923 None 0 Mouse Functional pIC50 = 6.9 6.9 -2 2
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 66923 None 0 Mouse Functional pIC50 = 6.9 6.9 -2 2
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 92920 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
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 92920 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
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 66192 None 0 Human Functional pIC50 = 5.9 5.9 10 2
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 66192 None 0 Human Functional pIC50 = 5.9 5.9 10 2
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 126892 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 126892 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 72122 None 2 Human Functional pIC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 72122 None 2 Human Functional pIC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 109421 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 109421 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 39452 None 6 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 39452 None 6 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 123943 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 123943 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 46572 None 10 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 46572 None 10 Human Functional pIC50 = 4.9 4.9 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 59803 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59803 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 93555 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 93555 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 172560 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 172560 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 142073 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 142073 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 109417 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 109417 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 59475 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59475 None 0 Human Functional pIC50 = 4.9 4.9 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 71975 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 71975 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 125929 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 125929 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 60662 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 60662 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 74905 None 0 Human Functional pIC50 = 7.9 7.9 123 2
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 74905 None 0 Human Functional pIC50 = 7.9 7.9 123 2
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 73502 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73502 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73643 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73643 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73648 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73648 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 19128 None 19 Human Functional pIC50 = 7.9 7.9 - 1
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 19128 None 19 Human Functional pIC50 = 7.9 7.9 - 1
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 71741 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 71741 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 71886 None 0 Human Functional pIC50 = 7.9 7.9 1 2
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 71886 None 0 Human Functional pIC50 = 7.9 7.9 1 2
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 19144 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 19144 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 60608 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 60608 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73169 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73169 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139108 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139108 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 138262 None 0 Human Functional pIC50 = 6.9 6.9 -2 2
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 138262 None 0 Human Functional pIC50 = 6.9 6.9 -2 2
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 92367 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 92367 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 123236 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 123236 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 69604 None 0 Human Functional pIC50 = 6.9 6.9 -61 3
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 69604 None 0 Human Functional pIC50 = 6.9 6.9 -61 3
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 93331 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
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 93331 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
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 80445 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 80445 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 73599 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73599 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 59718 None 0 Human Functional pIC50 = 4.9 4.9 -5 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59718 None 0 Human Functional pIC50 = 4.9 4.9 -5 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 16183 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 16183 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 125931 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125931 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125940 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125940 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 123738 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 123738 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 189408 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 189408 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73585 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 73585 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 60014 None 0 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60014 None 0 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73486 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73486 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 16225 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 16225 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 125934 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125934 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125947 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125947 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 78001 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 78001 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 23771 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23771 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 70585 None 0 Human Functional pIC50 = 5.8 5.8 -1412 11
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 70585 None 0 Human Functional pIC50 = 5.8 5.8 -1412 11
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 77967 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 77967 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 109383 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 109383 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 92413 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 92413 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 139277 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 139277 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 189409 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 189409 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73629 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73629 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 3632 None 13 Human Functional pIC50 = 7.8 7.8 - 1
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 3632 None 13 Human Functional pIC50 = 7.8 7.8 - 1
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 3632 None 13 Human Functional pIC50 = 7.8 7.8 - 1
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 71461 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 71461 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 81403 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 81403 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 142079 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 142079 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 60659 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60659 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 139239 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 139239 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73479 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73479 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 67229 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 67229 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 59378 None 0 Human Functional pIC50 = 5.8 5.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59378 None 0 Human Functional pIC50 = 5.8 5.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 54524 None 6 Human Functional pIC50 = 4.8 4.8 -1 4
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 54524 None 6 Human Functional pIC50 = 4.8 4.8 -1 4
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 38899 None 5 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 38899 None 5 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 60642 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 60642 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 60650 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 60650 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 16050 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 16050 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73532 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73532 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 56173 None 9 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56173 None 9 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56173 None 9 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 73488 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73488 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80080 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 80080 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 50092 None 11 Human Functional pIC50 = 4.8 4.8 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 50092 None 11 Human Functional pIC50 = 4.8 4.8 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51502 None 1 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51502 None 1 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 59337 None 0 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59337 None 0 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 26421 None 3 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 26421 None 3 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 199584 None 0 Human Functional pIC50 = 7.8 7.8 10 5
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 199584 None 0 Human Functional pIC50 = 7.8 7.8 10 5
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 82461 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 82461 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 129249 None 0 Human Functional pIC50 = 7.8 7.8 -5 2
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 129249 None 0 Human Functional pIC50 = 7.8 7.8 -5 2
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 73524 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73524 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 121830 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 121830 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 1899 None 38 Human Functional pIC50 = 7.8 7.8 - 1
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 1899 None 38 Human Functional pIC50 = 7.8 7.8 - 1
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 1899 None 38 Human Functional pIC50 = 7.8 7.8 - 1
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 73578 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73578 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73634 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73634 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 71748 None 0 Human Functional pIC50 = 7.8 7.8 1 3
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 71748 None 0 Human Functional pIC50 = 7.8 7.8 1 3
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 166471 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 166471 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 60600 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60600 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80250 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80250 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73484 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73484 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60653 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 60653 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 66727 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 66727 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 52893 None 6 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 52893 None 6 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 25432 None 5 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 25432 None 5 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 134874 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 134874 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73494 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73494 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 71658 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 71658 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 198919 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 198919 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 82519 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 82519 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 24701 None 4 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 24701 None 4 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51998 None 7 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51998 None 7 Human Functional pIC50 = 4.8 4.8 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80540 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80540 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80540 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80540 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 125111 None 3 Human Functional pIC50 = 5.8 5.8 - 1
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 33312 None 6 Human Functional pIC50 = 4.8 4.8 1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 33312 None 6 Human Functional pIC50 = 4.8 4.8 1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 123262 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 123262 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 64746 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 64746 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 64753 None 0 Human Functional pIC50 = 7.8 7.8 -12 3
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 64753 None 0 Human Functional pIC50 = 7.8 7.8 -12 3
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 56724 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 56724 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 194919 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 194919 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73626 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73626 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 60609 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60609 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60610 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60610 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60646 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60646 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73641 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73641 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 67231 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 67231 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166087 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166087 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 59637 None 0 Human Functional pIC50 = 5.8 5.8 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59637 None 0 Human Functional pIC50 = 5.8 5.8 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 51744 None 12 Human Functional pIC50 = 4.8 4.8 -7 3
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 51744 None 12 Human Functional pIC50 = 4.8 4.8 -7 3
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59616 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59616 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 166107 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166107 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 46696 None 6 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 46696 None 6 Human Functional pIC50 = 4.8 4.8 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125945 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125945 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 66990 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 66990 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 59750 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59750 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 56728 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 56728 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 93877 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 93877 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 55195 None 6 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55195 None 6 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55195 None 6 Human Functional pIC50 = 4.8 4.8 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125948 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 125948 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 80395 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 80395 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 139564 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
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 139564 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
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 64724 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 64724 None 0 Human Functional pIC50 = 7.8 7.8 1 2
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 56731 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 56731 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73499 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73499 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73637 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73637 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 16070 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 16070 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 81688 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 81688 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 68875 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 68875 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 68876 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 68876 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 60036 None 0 Human Functional pIC50 = 5.8 5.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60036 None 0 Human Functional pIC50 = 5.8 5.8 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73495 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73495 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 60739 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 60739 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 98276 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 98276 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 73596 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73596 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 140446 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 140446 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 59544 None 0 Human Functional pIC50 = 4.7 4.7 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59544 None 0 Human Functional pIC50 = 4.7 4.7 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 55908 None 2 Human Functional pIC50 = 4.7 4.7 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55908 None 2 Human Functional pIC50 = 4.7 4.7 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55908 None 2 Human Functional pIC50 = 4.7 4.7 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 16202 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 16202 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 40230 None 5 Human Functional pIC50 = 4.7 4.7 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 40230 None 5 Human Functional pIC50 = 4.7 4.7 2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 124119 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 124119 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 72395 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 72395 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 80455 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 80455 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 3727 None 22 Human Functional pIC50 = 7.7 7.7 -1 2
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 3727 None 22 Human Functional pIC50 = 7.7 7.7 -1 2
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 3727 None 22 Human Functional pIC50 = 7.7 7.7 -1 2
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 139157 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139157 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 138412 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 138412 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 56729 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 56729 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 198867 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 198867 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73646 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73646 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 132881 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 132881 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 80528 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 80528 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 80407 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 80407 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 92366 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 92366 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 151575 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 151575 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 66535 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 66535 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 72594 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 72594 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 80539 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 80539 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125946 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125946 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 77080 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 77080 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 67301 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 67301 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 21135 None 1 Human Functional pIC50 = 4.7 4.7 -3 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 21135 None 1 Human Functional pIC50 = 4.7 4.7 -3 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80527 None 25 Human Functional pIC50 = 6.7 6.7 - 1
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 80527 None 25 Human Functional pIC50 = 6.7 6.7 - 1
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 73577 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73577 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125936 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125936 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 149585 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 149585 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 38142 None 3 Human Functional pIC50 = 4.7 4.7 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 38142 None 3 Human Functional pIC50 = 4.7 4.7 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 80130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 168944 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 168944 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 141704 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 141704 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 200994 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 200994 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 76403 None 0 Human Functional pIC50 = 8.7 8.7 1 2
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 76403 None 0 Human Functional pIC50 = 8.7 8.7 1 2
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 80104 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 80104 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 80938 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 80938 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 199663 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 199663 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 74911 None 0 Human Functional pIC50 = 8.6 8.6 53 2
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 74911 None 0 Human Functional pIC50 = 8.6 8.6 53 2
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 96606 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 96606 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 201002 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 201002 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 80524 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 80524 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 80404 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 80404 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 76401 None 0 Human Functional pIC50 = 8.6 8.6 -1 2
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 76401 None 0 Human Functional pIC50 = 8.6 8.6 -1 2
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 142075 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 142075 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 74553 None 0 Human Functional pIC50 = 8.6 8.6 1 2
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 74553 None 0 Human Functional pIC50 = 8.6 8.6 1 2
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 68104 None 0 Human Functional pIC50 = 8.6 8.6 2 2
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 68104 None 0 Human Functional pIC50 = 8.6 8.6 2 2
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 74553 None 0 Human Functional pIC50 = 8.6 8.6 1 2
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 74553 None 0 Human Functional pIC50 = 8.6 8.6 1 2
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 199624 None 0 Human Functional pIC50 = 8.5 8.5 10 5
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 199624 None 0 Human Functional pIC50 = 8.5 8.5 10 5
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 2615 None 0 Human Functional pIC50 = 8.5 8.5 1 2
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 2615 None 0 Human Functional pIC50 = 8.5 8.5 1 2
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 2615 None 0 Human Functional pIC50 = 8.5 8.5 1 2
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 138976 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 138976 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179250 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 197764 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 197764 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73174 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73174 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 149847 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 149847 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 129251 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 129251 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 139155 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 139155 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 139159 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139159 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139206 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 139206 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 68877 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 68877 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 68879 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 68879 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73632 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73632 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 200014 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 200014 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 66227 None 0 Human Functional pIC50 = 7.7 7.7 776 2
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 66227 None 0 Human Functional pIC50 = 7.7 7.7 776 2
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 123952 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 123952 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 124807 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 124807 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 82246 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 82246 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76613 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76613 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 77091 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 77091 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 165925 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 165925 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 81185 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 81185 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 200896 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 200896 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 139266 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 139266 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 68869 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 68869 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 68870 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 68870 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 93256 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
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 93256 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
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 59446 None 0 Human Functional pIC50 = 5.7 5.7 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59446 None 0 Human Functional pIC50 = 5.7 5.7 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 69548 None 4 Human Functional pIC50 = 4.7 4.7 -19 2
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 69548 None 4 Human Functional pIC50 = 4.7 4.7 -19 2
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 59535 None 0 Human Functional pIC50 = 4.7 4.7 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59535 None 0 Human Functional pIC50 = 4.7 4.7 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 50502 None 1 Human Functional pIC50 = 4.7 4.7 -1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 50502 None 1 Human Functional pIC50 = 4.7 4.7 -1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 60645 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 60645 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 81586 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 81586 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 36345 None 10 Human Functional pIC50 = 4.7 4.7 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 36345 None 10 Human Functional pIC50 = 4.7 4.7 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125938 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125938 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 188151 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 188151 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139253 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 139253 None 0 Human Functional pIC50 = 7.7 7.7 -2 2
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 195697 None 0 Human Functional pIC50 = 7.7 7.7 407 2
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 195697 None 0 Human Functional pIC50 = 7.7 7.7 407 2
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 73639 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73639 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 199715 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 199715 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 65595 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 65595 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 59322 None 0 Human Functional pIC50 = 5.7 5.7 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59322 None 0 Human Functional pIC50 = 5.7 5.7 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 65595 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 65595 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 70401 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 70401 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 97095 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 97095 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 82173 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 82173 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 25888 None 4 Human Functional pIC50 = 4.7 4.7 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 25888 None 4 Human Functional pIC50 = 4.7 4.7 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 109387 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 109387 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 198288 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 198288 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125117 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 125117 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 26328 None 5 Human Functional pIC50 = 4.7 4.7 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 26328 None 5 Human Functional pIC50 = 4.7 4.7 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 184361 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 184361 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139195 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
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 139195 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
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 139240 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 139240 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 56721 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 56721 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 56733 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 56733 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 68103 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 68103 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 64668 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 64668 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 139186 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 139186 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 64726 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 64726 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 73593 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73593 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 124414 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 124414 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 124414 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 124414 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 60657 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 60657 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 59581 None 0 Human Functional pIC50 = 5.7 5.7 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59581 None 0 Human Functional pIC50 = 5.7 5.7 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 41860 None 11 Human Functional pIC50 = 4.7 4.7 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 41860 None 11 Human Functional pIC50 = 4.7 4.7 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125939 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125939 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 66275 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 66275 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73575 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73575 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 55867 None 24 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55867 None 24 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 55867 None 24 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125941 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 125941 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 66993 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 66993 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 36509 None 6 Human Functional pIC50 = 4.6 4.6 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 36509 None 6 Human Functional pIC50 = 4.6 4.6 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 86886 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 86886 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 87104 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 87104 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139097 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
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 139097 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
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 139147 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 139147 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 139248 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
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 139248 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
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 138335 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 138335 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 56738 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 56738 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 201374 None 24 Human Functional pIC50 = 7.6 7.6 - 1
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 201374 None 24 Human Functional pIC50 = 7.6 7.6 - 1
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 73601 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73601 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 19293 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 19293 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 201067 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 201067 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73592 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73592 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 92163 None 24 Rat Functional pIC50 = 6.6 6.6 - 1
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 92163 None 24 Rat Functional pIC50 = 6.6 6.6 - 1
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 60616 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 60616 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 94448 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 94448 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 29659 None 3 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 29659 None 3 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51744 None 12 Human Functional pIC50 = 4.6 4.6 -7 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51744 None 12 Human Functional pIC50 = 4.6 4.6 -7 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 37152 None 3 Human Functional pIC50 = 4.6 4.6 -15 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 37152 None 3 Human Functional pIC50 = 4.6 4.6 -15 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 24815 None 6 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 24815 None 6 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80228 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80228 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80357 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80357 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141734 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141734 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 60663 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 60663 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139400 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 139400 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
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 56732 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 56732 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73591 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73591 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 65228 None 0 Human Functional pIC50 = 6.6 6.6 91 2
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 65228 None 0 Human Functional pIC50 = 6.6 6.6 91 2
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 151032 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 151032 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 121829 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 121829 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 82328 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 82328 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 29837 None 13 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 29837 None 13 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 126266 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 126266 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 38426 None 5 Human Functional pIC50 = 4.6 4.6 -7 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 38426 None 5 Human Functional pIC50 = 4.6 4.6 -7 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 40413 None 4 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 40413 None 4 Human Functional pIC50 = 4.6 4.6 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 73477 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73477 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 201463 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
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 201463 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
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 82596 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 82596 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 199748 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 199748 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 3240 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 3240 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 3240 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139264 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139264 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73497 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73497 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 94364 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 94364 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 197995 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 197995 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 92547 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 92547 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 96643 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 96643 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 66156 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 66156 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141830 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141830 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141880 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 141880 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80055 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80055 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80953 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 80953 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 60644 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 60644 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 66278 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 66278 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 141917 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 141917 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 72472 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 72472 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 38587 None 3 Human Functional pIC50 = 4.6 4.6 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 38587 None 3 Human Functional pIC50 = 4.6 4.6 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 73590 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73590 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73598 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 73598 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 125950 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 125950 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 109423 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 109423 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 200977 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 200977 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 197834 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 197834 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139278 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139278 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73602 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73602 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73640 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73640 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 149809 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 149809 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 77297 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 77297 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 109418 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 109418 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 126450 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 126450 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 141392 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 141392 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 60612 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 60612 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 93283 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 93283 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 59574 None 0 Human Functional pIC50 = 5.6 5.6 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59574 None 0 Human Functional pIC50 = 5.6 5.6 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60651 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 60651 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 56229 None 0 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56229 None 0 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56229 None 0 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 82301 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 82301 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 60667 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 60667 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 192196 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 192196 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139038 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139038 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139257 None 30 Human Functional pIC50 = 7.6 7.6 -2 3
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 139257 None 30 Human Functional pIC50 = 7.6 7.6 -2 3
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 56588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 56588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73531 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73531 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73645 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73645 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 92340 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 92340 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 142312 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 142312 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 167459 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 167459 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
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 199297 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 199297 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 93556 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 93556 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 122724 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 122724 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 151031 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 151031 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 59362 None 0 Human Functional pIC50 = 5.6 5.6 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59362 None 0 Human Functional pIC50 = 5.6 5.6 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 29965 None 3 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 29965 None 3 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 169408 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 169408 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 46864 None 4 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 46864 None 4 Human Functional pIC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 139182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 139182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 98591 None 0 Human Functional pIC50 = 7.6 7.6 56 2
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 98591 None 0 Human Functional pIC50 = 7.6 7.6 56 2
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 70429 None 2 Human Functional pIC50 = 7.6 7.6 - 1
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 70429 None 2 Human Functional pIC50 = 7.6 7.6 - 1
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 72435 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 72435 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 135936 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
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 135936 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
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 16224 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 16224 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 62595 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 62595 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 33081 None 2 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 33081 None 2 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 141601 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 141601 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 198329 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 198329 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 149846 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 149846 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 139237 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 139237 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 64737 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 64737 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 76028 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76028 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 77380 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 77380 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66238 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 66238 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 72039 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 72039 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 59250 None 0 Human Functional pIC50 = 5.5 5.5 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59250 None 0 Human Functional pIC50 = 5.5 5.5 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59952 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59952 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 93513 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 93513 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 125928 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 125928 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73485 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73485 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 29210 None 3 Human Functional pIC50 = 4.5 4.5 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 29210 None 3 Human Functional pIC50 = 4.5 4.5 -5 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51659 None 2 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51659 None 2 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 109384 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 109384 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 109385 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 109385 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 194896 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 194896 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 194896 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73500 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73500 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 16223 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 16223 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 64955 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 64955 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80347 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80347 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80552 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80552 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80618 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80618 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80521 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80521 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81269 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81269 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81125 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81125 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80494 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80494 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81034 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 81034 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 76413 None 0 Human Functional pIC50 = 8.5 8.5 2 2
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 76413 None 0 Human Functional pIC50 = 8.5 8.5 2 2
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 141744 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 141744 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 76414 None 0 Human Functional pIC50 = 8.5 8.5 2 2
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 76414 None 0 Human Functional pIC50 = 8.5 8.5 2 2
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 82309 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 82309 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 141635 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 141635 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 80629 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 80629 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 76409 None 0 Human Functional pIC50 = 8.4 8.4 3 2
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 76409 None 0 Human Functional pIC50 = 8.4 8.4 3 2
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 80416 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 80416 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 79784 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 79784 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 139150 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
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 139150 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
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 56720 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 56720 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73487 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73487 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73597 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73597 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66162 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66162 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66180 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66180 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66269 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 66269 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 122990 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 122990 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 123720 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 123720 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 96707 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 96707 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 123647 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 123647 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 16222 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 16222 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 23879 None 11 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23879 None 11 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23879 None 11 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23879 None 11 Human Functional pIC50 = 4.5 4.5 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 73493 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73493 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 121828 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 121828 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 155366 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 155366 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 80311 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80311 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 60643 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 60643 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87956 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87956 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73481 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73481 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73636 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73636 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73638 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73638 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73651 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73651 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76029 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76029 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 82446 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 82446 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80285 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80285 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 141929 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 141929 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 166199 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 166199 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 60593 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 60593 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 59238 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59238 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59266 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59266 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59386 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59386 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59414 None 0 Human Functional pIC50 = 5.5 5.5 -11 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59414 None 0 Human Functional pIC50 = 5.5 5.5 -11 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59657 None 0 Human Functional pIC50 = 5.5 5.5 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59657 None 0 Human Functional pIC50 = 5.5 5.5 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 166169 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166169 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 123749 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 123749 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 60661 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 60661 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 81607 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 81607 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 138754 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 138754 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 51912 None 2 Human Functional pIC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 51912 None 2 Human Functional pIC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 60613 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 60613 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 73501 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73501 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 179294 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 179294 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73600 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73600 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 142676 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 142676 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 60614 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 60614 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 47200 None 5 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 47200 None 5 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 80306 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80306 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 64736 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 64736 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 139560 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 139560 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
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 73483 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73483 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73530 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73530 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 68872 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 68872 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 59219 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59219 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59399 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59399 None 0 Human Functional pIC50 = 5.5 5.5 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 23776 None 4 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 23776 None 4 Human Functional pIC50 = 4.5 4.5 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 52327 None 5 Human Functional pIC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 52327 None 5 Human Functional pIC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 109425 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 109425 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 139141 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
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 139141 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
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 139225 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
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 139225 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
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 56717 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 56717 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 68096 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 68096 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73644 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73644 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73649 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73649 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 92623 None 1 Rat Functional pIC50 = 7.5 7.5 - 1
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 92623 None 1 Rat Functional pIC50 = 7.5 7.5 - 1
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 76551 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76551 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 64722 None 0 Human Functional pIC50 = 6.5 6.5 1 2
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 64722 None 0 Human Functional pIC50 = 6.5 6.5 1 2
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 73572 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73572 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 66157 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 66157 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 71899 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 71899 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 59199 None 0 Human Functional pIC50 = 5.5 5.5 -8 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59199 None 0 Human Functional pIC50 = 5.5 5.5 -8 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 65342 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 65342 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 66215 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 66215 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 80229 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80229 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 139064 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 139064 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 154785 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 154785 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73603 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73603 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73635 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73635 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80366 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 80366 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 60649 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 60649 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73478 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73478 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73490 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73490 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 93332 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 93332 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 166446 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166446 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 59758 None 0 Human Functional pIC50 = 5.5 5.5 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59758 None 0 Human Functional pIC50 = 5.5 5.5 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 46452 None 8 Human Functional pIC50 = 4.4 4.4 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 46452 None 8 Human Functional pIC50 = 4.4 4.4 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 141565 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 141565 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60611 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 60611 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 92162 None 1 Rat Functional pIC50 = 6.4 6.4 - 1
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 92162 None 1 Rat Functional pIC50 = 6.4 6.4 - 1
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 67039 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 67039 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 97438 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 97438 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 109429 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 109429 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 64728 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 64728 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 16238 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 16238 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 59136 None 0 Human Functional pIC50 = 5.4 5.4 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59136 None 0 Human Functional pIC50 = 5.4 5.4 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59431 None 0 Human Functional pIC50 = 5.4 5.4 -5 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59431 None 0 Human Functional pIC50 = 5.4 5.4 -5 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 141994 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 141994 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 72458 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 72458 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 67153 None 0 Mouse Functional pIC50 = 6.4 6.4 -4 2
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 67153 None 0 Mouse Functional pIC50 = 6.4 6.4 -4 2
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 60607 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 60607 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73170 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73170 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73475 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73475 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73527 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73527 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 109428 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 109428 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73631 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73631 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 82452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 59374 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59374 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59876 None 0 Human Functional pIC50 = 5.4 5.4 -14 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59876 None 0 Human Functional pIC50 = 5.4 5.4 -14 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59985 None 0 Human Functional pIC50 = 5.4 5.4 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59985 None 0 Human Functional pIC50 = 5.4 5.4 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 141644 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 141644 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 165869 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 165869 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 199824 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 199824 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 76412 None 0 Human Functional pIC50 = 8.4 8.4 2 2
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 76412 None 0 Human Functional pIC50 = 8.4 8.4 2 2
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 73506 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73506 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73525 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73525 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 68883 None 0 Rat Functional pIC50 = 8.4 8.4 -2 2
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 68883 None 0 Rat Functional pIC50 = 8.4 8.4 -2 2
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 82322 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 82322 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 74918 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 74918 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 76402 None 0 Human Functional pIC50 = 8.4 8.4 -1 2
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 76402 None 0 Human Functional pIC50 = 8.4 8.4 -1 2
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 1158 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 1158 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 1158 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 199706 None 0 Human Functional pIC50 = 8.3 8.3 26 4
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 199706 None 0 Human Functional pIC50 = 8.3 8.3 26 4
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 64738 None 0 Human Functional pIC50 = 8.3 8.3 -1 2
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 64738 None 0 Human Functional pIC50 = 8.3 8.3 -1 2
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 80313 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80313 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 82308 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82308 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139263 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139263 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 74870 None 0 Human Functional pIC50 = 7.4 7.4 3 2
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 74870 None 0 Human Functional pIC50 = 7.4 7.4 3 2
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 73573 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73573 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 65236 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 65236 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 68871 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 68871 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73171 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73171 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 59920 None 0 Human Functional pIC50 = 5.4 5.4 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59920 None 0 Human Functional pIC50 = 5.4 5.4 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73522 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73522 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 93911 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 93911 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 78065 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 78065 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60655 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60655 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 66626 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 66626 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82172 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82172 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 135667 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 135667 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60606 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 60606 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 59324 None 0 Human Functional pIC50 = 5.4 5.4 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59324 None 0 Human Functional pIC50 = 5.4 5.4 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 142055 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 142055 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 109420 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 109420 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 73595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 81521 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 81521 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 80403 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 80403 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 138371 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 138371 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 94063 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 94063 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 80662 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 80662 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 168826 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 168826 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 71485 None 0 Human Functional pIC50 = 7.4 7.4 -1 3
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 71485 None 0 Human Functional pIC50 = 7.4 7.4 -1 3
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 93467 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 93467 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 109431 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 109431 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139262 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139262 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 3727 None 22 Human Functional pIC50 = 7.4 7.4 -1 2
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 3727 None 22 Human Functional pIC50 = 7.4 7.4 -1 2
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 3727 None 22 Human Functional pIC50 = 7.4 7.4 -1 2
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 64725 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 64725 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 73633 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73633 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 138569 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 138569 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60665 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 60665 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87287 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87287 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139236 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139236 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 123656 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 123656 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 93226 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
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 93226 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
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 70441 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 70441 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73173 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73173 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 82453 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 82453 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 129255 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
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 129255 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
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 73489 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73489 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73642 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73642 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 16098 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 16098 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82510 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 82510 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 179083 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 179083 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 71973 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 71973 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 65595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 65595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 76087 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 76087 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 199745 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 199745 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 126432 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 126432 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 60656 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 60656 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 59771 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59771 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 133509 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 133509 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 123241 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 123241 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 109422 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 109422 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 64639 None 0 Human Functional pIC50 = 7.3 7.3 -1 2
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 64639 None 0 Human Functional pIC50 = 7.3 7.3 -1 2
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 59130 None 0 Human Functional pIC50 = 5.3 5.3 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59130 None 0 Human Functional pIC50 = 5.3 5.3 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 79124 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 79124 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 40695 None 3 Human Functional pIC50 = 5.3 5.3 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 40695 None 3 Human Functional pIC50 = 5.3 5.3 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 82855 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 82855 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 186841 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 186841 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 93427 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 93427 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 60615 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 60615 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 59142 None 0 Human Functional pIC50 = 5.3 5.3 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59142 None 0 Human Functional pIC50 = 5.3 5.3 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 56726 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 56726 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 16048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 16048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 72016 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 72016 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 81671 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 81671 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 199343 None 0 Human Functional pIC50 = 8.3 8.3 61 5
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 199343 None 0 Human Functional pIC50 = 8.3 8.3 61 5
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 151505 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 151505 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141992 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141992 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80597 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80597 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80622 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80622 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80874 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80874 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141520 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141520 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141540 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141540 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141751 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141751 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 142039 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 142039 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80079 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 80079 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 169093 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 169093 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 71895 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 71895 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 142048 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 142048 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 68110 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 68110 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 68106 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 68106 None 0 Human Functional pIC50 = 8.3 8.3 1 2
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 3727 None 22 Human Functional pIC50 = 8.3 8.3 -1 2
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 3727 None 22 Human Functional pIC50 = 8.3 8.3 -1 2
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 3727 None 22 Human Functional pIC50 = 8.3 8.3 -1 2
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 82584 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 82584 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 201374 None 24 Human Functional pIC50 = 8.3 8.3 - 1
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 201374 None 24 Human Functional pIC50 = 8.3 8.3 - 1
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 82455 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 82455 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 64739 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 64739 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 139255 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 139255 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 68873 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 68873 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 68884 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 68884 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 76132 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 76132 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 123658 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 123658 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 59272 None 0 Human Functional pIC50 = 5.3 5.3 -7 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59272 None 0 Human Functional pIC50 = 5.3 5.3 -7 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59707 None 0 Human Functional pIC50 = 5.3 5.3 3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59707 None 0 Human Functional pIC50 = 5.3 5.3 3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 141641 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 141641 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 142077 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 142077 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 177070 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 177070 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 123907 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 123907 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 141630 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 141630 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 93512 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 93512 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 81621 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 81621 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 140599 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 140599 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 71898 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 71898 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 133500 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 133500 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 80393 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 80393 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 66261 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 66261 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 109386 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 109386 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 109432 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 109432 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 93352 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 93352 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 140670 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 140670 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 172560 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 172560 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 66936 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 66936 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 60601 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 60601 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 66246 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 66246 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 66749 None 0 Mouse Functional pIC50 = 6.3 6.3 -5 2
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 66749 None 0 Mouse Functional pIC50 = 6.3 6.3 -5 2
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 67529 None 0 Mouse Functional pIC50 = 6.3 6.3 -17 2
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 67529 None 0 Mouse Functional pIC50 = 6.3 6.3 -17 2
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 125388 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 125388 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 67000 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 67000 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 73505 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73505 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73587 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73587 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 16125 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 16125 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 66898 None 0 Mouse Functional pIC50 = 6.3 6.3 -6 2
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 66898 None 0 Mouse Functional pIC50 = 6.3 6.3 -6 2
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 93282 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
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 93282 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
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 59864 None 0 Human Functional pIC50 = 5.3 5.3 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59864 None 0 Human Functional pIC50 = 5.3 5.3 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59869 None 0 Human Functional pIC50 = 5.3 5.3 -9 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59869 None 0 Human Functional pIC50 = 5.3 5.3 -9 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 93466 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 93466 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 80303 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 80303 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73534 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73534 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 138384 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 138384 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 71954 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 71954 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 59163 None 0 Human Functional pIC50 = 5.3 5.3 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59163 None 0 Human Functional pIC50 = 5.3 5.3 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73650 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73650 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 72529 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 72529 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 67104 None 0 Mouse Functional pIC50 = 6.3 6.3 -11 2
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 67104 None 0 Mouse Functional pIC50 = 6.3 6.3 -11 2
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 16250 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 16250 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 73594 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73594 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 144574 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 144574 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 92899 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 92899 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 59728 None 0 Human Functional pIC50 = 5.2 5.2 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59728 None 0 Human Functional pIC50 = 5.2 5.2 - 1
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59900 None 0 Human Functional pIC50 = 5.2 5.2 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59900 None 0 Human Functional pIC50 = 5.2 5.2 -4 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73584 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 73584 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 80358 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80358 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199664 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199664 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 174464 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 174464 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 81604 None 0 Human Functional pIC50 = 7.2 7.2 15 2
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 81604 None 0 Human Functional pIC50 = 7.2 7.2 15 2
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 68874 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 68874 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 66267 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 66267 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 59428 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59428 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60002 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60002 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 141587 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 141587 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 70308 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 70308 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 67017 None 0 Human Functional pIC50 = 5.2 5.2 3 2
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 67017 None 0 Human Functional pIC50 = 5.2 5.2 3 2
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 77938 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77938 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80212 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80212 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 109433 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 109433 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 198519 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 198519 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73528 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73528 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73536 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73536 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 154898 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 154898 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80263 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 80263 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 199248 None 0 Human Functional pIC50 = 8.2 8.2 50 5
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 199248 None 0 Human Functional pIC50 = 8.2 8.2 50 5
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 68882 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 68882 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 68883 None 0 Human Functional pIC50 = 8.2 8.2 2 2
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 68883 None 0 Human Functional pIC50 = 8.2 8.2 2 2
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 73647 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73647 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 80413 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 80413 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 3849 None 3 Rat Functional pIC50 = 8.2 8.2 1 2
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 3849 None 3 Rat Functional pIC50 = 8.2 8.2 1 2
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 3849 None 3 Rat Functional pIC50 = 8.2 8.2 1 2
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 81134 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 81134 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 68171 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 68171 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 80576 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 80576 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 80847 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 80847 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141561 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141561 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141642 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141642 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141670 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141670 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 79865 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 79865 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141514 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141514 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 76411 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 76411 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 76418 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 76418 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 199747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 199747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 64733 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 64733 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
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 76422 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 76422 None 0 Human Functional pIC50 = 8.2 8.2 1 2
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 78068 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 78068 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 133657 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 133657 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199661 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 199661 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 16123 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 16123 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 92544 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 92544 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 65503 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 65503 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 82515 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 82515 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 66230 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 66230 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 139259 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139259 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73503 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 73503 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 59938 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59938 None 0 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73582 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73582 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80712 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 80712 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77152 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77152 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 92548 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 92548 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 133224 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 133224 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 141681 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 141681 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 124163 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 124163 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 81131 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 81131 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73583 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73583 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 124395 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 124395 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 67073 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 67073 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 59365 None 0 Human Functional pIC50 = 5.2 5.2 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59365 None 0 Human Functional pIC50 = 5.2 5.2 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60069 None 0 Human Functional pIC50 = 5.2 5.2 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60069 None 0 Human Functional pIC50 = 5.2 5.2 -3 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 16149 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 16149 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 199739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 60654 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 60654 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 135550 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 135550 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 27839 None 10 Human Functional pIC50 = 4.2 4.2 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 27839 None 10 Human Functional pIC50 = 4.2 4.2 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 16203 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 16203 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 64721 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
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 64721 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
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 16097 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 16097 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 93225 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 93225 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 69636 None 0 Human Functional pIC50 = 7.2 7.2 75 2
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 69636 None 0 Human Functional pIC50 = 7.2 7.2 75 2
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 56185 None 3 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56185 None 3 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56185 None 3 Human Functional pIC50 = 5.2 5.2 1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 109430 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 109430 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77093 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77093 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 70332 None 0 Human Functional pIC50 = 7.2 7.2 -3 2
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 70332 None 0 Human Functional pIC50 = 7.2 7.2 -3 2
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 98740 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 98740 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73533 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73533 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 189247 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 189247 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 60602 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 60602 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 92173 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 92173 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 59283 None 0 Human Functional pIC50 = 5.2 5.2 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59283 None 0 Human Functional pIC50 = 5.2 5.2 -6 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 66926 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 66926 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 77354 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77354 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 59979 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59979 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60024 None 0 Human Functional pIC50 = 5.2 5.2 2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60024 None 0 Human Functional pIC50 = 5.2 5.2 2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 81052 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 81052 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 82478 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 82478 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 179189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 179189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 60652 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 60652 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 74917 None 0 Human Functional pIC50 = 8.2 8.2 213 2
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 74917 None 0 Human Functional pIC50 = 8.2 8.2 213 2
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 68881 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 68881 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 64955 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 64955 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 66262 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 66262 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 511 None 14 Human Functional pIC50 = 8.1 8.1 2 7
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 511 None 14 Human Functional pIC50 = 8.1 8.1 2 7
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 511 None 14 Human Functional pIC50 = 8.1 8.1 2 7
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 68105 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 68105 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 71220 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 71220 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 199622 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 199622 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 74920 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 74920 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80433 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80433 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80024 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80024 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 64753 None 0 Human Functional pIC50 = 8.1 8.1 -12 3
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 64753 None 0 Human Functional pIC50 = 8.1 8.1 -12 3
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 80427 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80427 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80941 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 80941 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 60599 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 60599 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199062 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199062 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139040 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139040 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 66172 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 66172 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 71875 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 71875 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 68865 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 68865 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 59555 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59555 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 142074 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 142074 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139192 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139192 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 173234 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 173234 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 16068 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 16068 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 122619 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 122619 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 142678 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 142678 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 149496 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
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 149496 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
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 77089 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 77089 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 93363 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
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 93363 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
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 124169 None 0 Mouse Functional pIC50 = 6.1 6.1 -12 2
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 124169 None 0 Mouse Functional pIC50 = 6.1 6.1 -12 2
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 60053 None 0 Human Functional pIC50 = 6.1 6.1 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 60053 None 0 Human Functional pIC50 = 6.1 6.1 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 76557 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 76557 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 192462 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 192462 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73574 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73574 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73576 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73576 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 71783 None 0 Human Functional pIC50 = 7.1 7.1 -4 3
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 71783 None 0 Human Functional pIC50 = 7.1 7.1 -4 3
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 59494 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59494 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 139158 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 139158 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 59437 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59437 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 16184 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 16184 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 127238 None 0 Mouse Functional pIC50 = 6.1 6.1 -15 2
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 127238 None 0 Mouse Functional pIC50 = 6.1 6.1 -15 2
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 82484 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 82484 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 125942 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 125942 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 93990 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 93990 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 125949 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 125949 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 82426 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 82426 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 80371 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 80371 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 82577 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 82577 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121334 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
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 121334 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
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 124452 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 124452 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 80943 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 80943 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 16096 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 16096 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 201210 None 0 Human Functional pIC50 = 8.1 8.1 25 4
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 201210 None 0 Human Functional pIC50 = 8.1 8.1 25 4
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 94213 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 94213 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 66221 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 66221 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 169042 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 169042 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 74915 None 0 Human Functional pIC50 = 8.1 8.1 81 2
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 74915 None 0 Human Functional pIC50 = 8.1 8.1 81 2
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 142025 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 142025 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 74900 None 0 Human Functional pIC50 = 8.1 8.1 251 2
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 74900 None 0 Human Functional pIC50 = 8.1 8.1 251 2
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 109426 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 109426 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73504 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73504 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 59403 None 0 Human Functional pIC50 = 5.1 5.1 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59403 None 0 Human Functional pIC50 = 5.1 5.1 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 37780 None 24 Human Functional pIC50 = 5.1 5.1 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 37780 None 24 Human Functional pIC50 = 5.1 5.1 -2 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 189937 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 189937 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 200830 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 200830 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73507 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73507 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 109419 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 109419 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 124420 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 124420 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 82514 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 82514 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 59268 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59268 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 73526 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 73526 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 75803 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75803 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 94577 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 94577 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73580 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73580 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 189484 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 189484 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 141583 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 141583 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 60647 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 60647 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 59679 None 0 Human Functional pIC50 = 5.1 5.1 -23 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59679 None 0 Human Functional pIC50 = 5.1 5.1 -23 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 47998 None 4 Human Functional pIC50 = 5.1 5.1 1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 47998 None 4 Human Functional pIC50 = 5.1 5.1 1 3
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 125943 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 125943 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 199003 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 199003 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 94511 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 94511 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 16069 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 16069 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 16124 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 16124 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 93991 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 93991 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73586 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73586 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 67193 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 67193 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 80592 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 80592 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 3727 None 22 Human Functional pIC50 = 6.1 6.1 -1 2
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 3727 None 22 Human Functional pIC50 = 6.1 6.1 -1 2
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 3727 None 22 Human Functional pIC50 = 6.1 6.1 -1 2
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 63263 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 63263 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 16126 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 16126 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 138783 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 138783 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 71122 None 0 Human Functional pIC50 = 7.1 7.1 38 2
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 71122 None 0 Human Functional pIC50 = 7.1 7.1 38 2
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 66258 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 66258 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 73588 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73588 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 67206 None 2 Human Functional pIC50 = 7.1 7.1 31 2
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 67206 None 2 Human Functional pIC50 = 7.1 7.1 31 2
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 1899 None 38 Human Functional pIC50 = 7.1 7.1 - 1
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 1899 None 38 Human Functional pIC50 = 7.1 7.1 - 1
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 1899 None 38 Human Functional pIC50 = 7.1 7.1 - 1
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 67002 None 0 Mouse Functional pIC50 = 6.1 6.1 -44 2
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 67002 None 0 Mouse Functional pIC50 = 6.1 6.1 -44 2
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 123866 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 123866 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 60664 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 60664 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 142898 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 142898 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 74868 None 0 Human Functional pIC50 = 8.1 8.1 46 2
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 74868 None 0 Human Functional pIC50 = 8.1 8.1 46 2
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 73498 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 73498 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 16251 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 16251 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 81833 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 81833 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 165875 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 165875 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 74871 None 0 Human Functional pIC50 = 8.0 8.0 30 2
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 74871 None 0 Human Functional pIC50 = 8.0 8.0 30 2
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 68109 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 68109 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 64723 None 0 Human Functional pIC50 = 8.0 8.0 1 2
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 141525 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 141525 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 199659 None 1 Human Functional pIC50 = 8.0 8.0 - 1
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 199659 None 1 Human Functional pIC50 = 8.0 8.0 - 1
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 161377 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 161377 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 79764 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 79764 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 198424 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 198424 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 154722 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 154722 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 179273 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 179273 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 65595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 65595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 65595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 65595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 67447 None 0 Mouse Functional pIC50 = 7.1 7.1 -29 2
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 67447 None 0 Mouse Functional pIC50 = 7.1 7.1 -29 2
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 166076 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 166076 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 60660 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 60660 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 64719 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 64719 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 73482 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73482 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73589 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73589 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 66226 None 0 Human Functional pIC50 = 5.0 5.0 - 1
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 66226 None 0 Human Functional pIC50 = 5.0 5.0 - 1
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 179169 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 179169 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 72133 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 72133 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 139272 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 139272 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16127 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16127 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 132819 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 132819 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 56038 None 6 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56038 None 6 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 56038 None 6 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 198751 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 198751 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 199017 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 199017 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 60648 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 60648 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 81083 None 2 Human Functional pIC50 = 6.0 6.0 - 1
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 81083 None 2 Human Functional pIC50 = 6.0 6.0 - 1
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 59488 None 0 Human Functional pIC50 = 5.0 5.0 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59488 None 0 Human Functional pIC50 = 5.0 5.0 1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 141680 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 141680 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 109434 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 109434 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16201 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16201 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 141829 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 141829 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81603 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 81603 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 154704 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 154704 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 16186 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 16186 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 16249 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 16249 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 70198 None 0 Human Functional pIC50 = 7.0 7.0 851 2
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 70198 None 0 Human Functional pIC50 = 7.0 7.0 851 2
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 59557 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 59557 None 0 Human Functional pIC50 = 5.0 5.0 -1 2
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists 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 31307 None 9 Human Functional pIC50 = 5 5.0 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 31307 None 9 Human Functional pIC50 = 5 5.0 - 1
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class 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 3632 None 13 Human Functional pKd = 9.2 9.2 - 1
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 3632 None 13 Human Functional pKd = 9.2 9.2 - 1
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 3632 None 13 Human Functional pKd = 9.2 9.2 - 1
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 81597 None 0 Human Functional pKd = 8 8.0 -2 3
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 81597 None 0 Human Functional pKd = 8 8.0 -2 3
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 140260 None 0 Human Functional pKi = 9 9.0 - 0
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 140260 None 0 Human Functional pKi = 9 9.0 - 0
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 17056 None 0 Human Functional pKi = 8.9 8.9 - 0
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 17056 None 0 Human Functional pKi = 8.9 8.9 - 0
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 138490 None 0 Human Functional pKi = 8.9 8.9 - 0
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 138490 None 0 Human Functional pKi = 8.9 8.9 - 0
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 17041 None 0 Human Functional pKi = 8.8 8.8 - 0
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 17041 None 0 Human Functional pKi = 8.8 8.8 - 0
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 17042 None 0 Human Functional pKi = 8.8 8.8 - 0
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 17042 None 0 Human Functional pKi = 8.8 8.8 - 0
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 79895 None 0 Human Functional pKi = 8.8 8.8 - 0
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 79895 None 0 Human Functional pKi = 8.8 8.8 - 0
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 17048 None 0 Human Functional pKi = 8.7 8.7 - 0
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 17048 None 0 Human Functional pKi = 8.7 8.7 - 0
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 72607 None 0 Human Functional pKi = 8 8.0 - 0
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 72607 None 0 Human Functional pKi = 8 8.0 - 0
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 97325 None 0 Human Functional pKi = 8 8.0 - 0
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 97325 None 0 Human Functional pKi = 8 8.0 - 0
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 138499 None 0 Human Functional pKi = 8.0 8.0 - 0
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 138499 None 0 Human Functional pKi = 8.0 8.0 - 0
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 167563 None 0 Human Functional pKi = 8.0 8.0 - 1
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 167563 None 0 Human Functional pKi = 8.0 8.0 - 1
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 17047 None 0 Human Functional pKi = 8.0 8.0 - 0
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 17047 None 0 Human Functional pKi = 8.0 8.0 - 0
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 17055 None 0 Human Functional pKi = 8.0 8.0 - 0
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 17055 None 0 Human Functional pKi = 8.0 8.0 - 0
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 17082 None 0 Human Functional pKi = 8.0 8.0 - 0
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 17082 None 0 Human Functional pKi = 8.0 8.0 - 0
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 81578 None 0 Human Functional pKi = 4 4.0 - 0
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 81578 None 0 Human Functional pKi = 4 4.0 - 0
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 96470 None 0 Human Functional pKi = 7.0 7.0 - 0
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 96470 None 0 Human Functional pKi = 7.0 7.0 - 0
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 89359 None 0 Human Functional pKi = 7.0 7.0 - 0
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 89359 None 0 Human Functional pKi = 7.0 7.0 - 0
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 80904 None 0 Human Functional pKi = 8.0 8.0 - 1
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 80904 None 0 Human Functional pKi = 8.0 8.0 - 1
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 82504 None 0 Human Functional pKi = 8.0 8.0 - 1
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 82504 None 0 Human Functional pKi = 8.0 8.0 - 1
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 17035 None 0 Human Functional pKi = 7.9 7.9 - 0
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 17035 None 0 Human Functional pKi = 7.9 7.9 - 0
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 85821 None 0 Human Functional pKi = 6.9 6.9 - 0
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 85821 None 0 Human Functional pKi = 6.9 6.9 - 0
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 145330 None 0 Human Functional pKi = 6.9 6.9 - 0
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 145330 None 0 Human Functional pKi = 6.9 6.9 - 0
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 81796 None 0 Human Functional pKi = 6.9 6.9 - 1
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 81796 None 0 Human Functional pKi = 6.9 6.9 - 1
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 133635 None 0 Human Functional pKi = 7.9 7.9 - 0
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 133635 None 0 Human Functional pKi = 7.9 7.9 - 0
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 82585 None 0 Human Functional pKi = 7.9 7.9 - 1
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 82585 None 0 Human Functional pKi = 7.9 7.9 - 1
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 138982 None 0 Human Functional pKi = 6.9 6.9 - 0
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 138982 None 0 Human Functional pKi = 6.9 6.9 - 0
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 139612 None 0 Human Functional pKi = 6.9 6.9 - 0
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 139612 None 0 Human Functional pKi = 6.9 6.9 - 0
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 168924 None 0 Human Functional pKi = 6.9 6.9 - 0
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 168924 None 0 Human Functional pKi = 6.9 6.9 - 0
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 81597 None 0 Human Functional pKi = 7.9 7.9 -2 3
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 81597 None 0 Human Functional pKi = 7.9 7.9 -2 3
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 81597 None 0 Rat Functional pKi = 7.9 7.9 1 3
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 81597 None 0 Rat Functional pKi = 7.9 7.9 1 3
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 17016 None 0 Human Functional pKi = 7.9 7.9 - 0
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 17016 None 0 Human Functional pKi = 7.9 7.9 - 0
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 142387 None 0 Human Functional pKi = 7.9 7.9 - 0
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 142387 None 0 Human Functional pKi = 7.9 7.9 - 0
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 142387 None 0 Human Functional pKi = 7.9 7.9 - 0
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 142387 None 0 Human Functional pKi = 7.9 7.9 - 0
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 77792 None 0 Human Functional pKi = 7.9 7.9 - 0
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 77792 None 0 Human Functional pKi = 7.9 7.9 - 0
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 89648 None 0 Human Functional pKi = 7.9 7.9 - 0
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 89648 None 0 Human Functional pKi = 7.9 7.9 - 0
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 72434 None 0 Human Functional pKi = 6.9 6.9 - 0
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 72434 None 0 Human Functional pKi = 6.9 6.9 - 0
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 138981 None 0 Human Functional pKi = 6.9 6.9 - 1
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 138981 None 0 Human Functional pKi = 6.9 6.9 - 1
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 17124 None 0 Human Functional pKi = 6.9 6.9 - 0
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 17124 None 0 Human Functional pKi = 6.9 6.9 - 0
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 79894 None 0 Human Functional pKi = 6.9 6.9 - 1
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 79894 None 0 Human Functional pKi = 6.9 6.9 - 1
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 16960 None 0 Human Functional pKi = 6.9 6.9 - 0
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 16960 None 0 Human Functional pKi = 6.9 6.9 - 0
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 81597 None 0 Mouse Functional pKi = 7.9 7.9 -1 3
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 81597 None 0 Mouse Functional pKi = 7.9 7.9 -1 3
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 77961 None 0 Human Functional pKi = 7.9 7.9 - 0
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 77961 None 0 Human Functional pKi = 7.9 7.9 - 0
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 97135 None 0 Human Functional pKi = 6.9 6.9 - 1
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 97135 None 0 Human Functional pKi = 6.9 6.9 - 1
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 80020 None 0 Human Functional pKi = 6.9 6.9 - 0
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 80020 None 0 Human Functional pKi = 6.9 6.9 - 0
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 78339 None 0 Human Functional pKi = 5.8 5.8 - 0
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 78339 None 0 Human Functional pKi = 5.8 5.8 - 0
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 80346 None 0 Human Functional pKi = 6.8 6.8 - 0
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 80346 None 0 Human Functional pKi = 6.8 6.8 - 0
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 165950 None 0 Human Functional pKi = 6.8 6.8 - 1
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 165950 None 0 Human Functional pKi = 6.8 6.8 - 1
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 85812 None 0 Human Functional pKi = 6.8 6.8 - 0
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 85812 None 0 Human Functional pKi = 6.8 6.8 - 0
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 82329 None 0 Human Functional pKi = 6.8 6.8 - 1
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 82329 None 0 Human Functional pKi = 6.8 6.8 - 1
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 72506 None 0 Human Functional pKi = 7.8 7.8 - 0
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 72506 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16945 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16945 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16988 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16988 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17018 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17018 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17054 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17054 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17071 None 0 Human Functional pKi = 7.8 7.8 - 0
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 17071 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54992 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54992 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54992 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78037 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78037 None 0 Human Functional pKi = 7.8 7.8 - 0
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 79799 None 0 Human Functional pKi = 7.8 7.8 - 0
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 79799 None 0 Human Functional pKi = 7.8 7.8 - 0
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 172857 None 0 Human Functional pKi = 7.8 7.8 - 0
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 172857 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78423 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78423 None 0 Human Functional pKi = 7.8 7.8 - 0
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 82613 None 0 Human Functional pKi = 4.8 4.8 - 0
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 82613 None 0 Human Functional pKi = 4.8 4.8 - 0
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 71972 None 0 Human Functional pKi = 6.8 6.8 - 0
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 71972 None 0 Human Functional pKi = 6.8 6.8 - 0
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 72579 None 0 Human Functional pKi = 6.8 6.8 - 0
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 72579 None 0 Human Functional pKi = 6.8 6.8 - 0
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 71880 None 0 Human Functional pKi = 7.8 7.8 - 0
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 71880 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54994 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54994 None 0 Human Functional pKi = 7.8 7.8 - 0
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 54994 None 0 Human Functional pKi = 7.8 7.8 - 0
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 77340 None 0 Human Functional pKi = 7.8 7.8 - 0
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 77340 None 0 Human Functional pKi = 7.8 7.8 - 0
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 139600 None 0 Human Functional pKi = 7.8 7.8 - 0
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 139600 None 0 Human Functional pKi = 7.8 7.8 - 0
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 169447 None 0 Human Functional pKi = 7.8 7.8 - 0
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 169447 None 0 Human Functional pKi = 7.8 7.8 - 0
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 141970 None 0 Human Functional pKi = 4.8 4.8 - 0
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 141970 None 0 Human Functional pKi = 4.8 4.8 - 0
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 93701 None 0 Human Functional pKi = 6.8 6.8 - 0
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 93701 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78131 None 0 Human Functional pKi = 5.8 5.8 - 0
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 78131 None 0 Human Functional pKi = 5.8 5.8 - 0
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 169477 None 0 Human Functional pKi = 6.8 6.8 - 0
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 169477 None 0 Human Functional pKi = 6.8 6.8 - 0
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 89551 None 0 Human Functional pKi = 7.8 7.8 - 0
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 89551 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16981 None 0 Human Functional pKi = 7.8 7.8 - 0
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 16981 None 0 Human Functional pKi = 7.8 7.8 - 0
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 169498 None 0 Human Functional pKi = 6.8 6.8 - 0
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 169498 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78648 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78648 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78160 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78160 None 0 Human Functional pKi = 6.8 6.8 - 0
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 72513 None 0 Human Functional pKi = 7.8 7.8 - 0
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 72513 None 0 Human Functional pKi = 7.8 7.8 - 0
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 138752 None 0 Human Functional pKi = 7.8 7.8 - 0
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 138752 None 0 Human Functional pKi = 7.8 7.8 - 0
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 82168 None 0 Human Functional pKi = 7.8 7.8 - 1
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 82168 None 0 Human Functional pKi = 7.8 7.8 - 1
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 78198 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78198 None 0 Human Functional pKi = 6.8 6.8 - 0
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 17072 None 0 Human Functional pKi = 6.7 6.7 - 0
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 17072 None 0 Human Functional pKi = 6.7 6.7 - 0
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 81620 None 0 Human Functional pKi = 6.7 6.7 - 1
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 81620 None 0 Human Functional pKi = 6.7 6.7 - 1
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 72373 None 0 Human Functional pKi = 7.7 7.7 - 0
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 72373 None 0 Human Functional pKi = 7.7 7.7 - 0
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 148742 None 0 Human Functional pKi = 7.7 7.7 - 0
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 148742 None 0 Human Functional pKi = 7.7 7.7 - 0
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 79913 None 0 Human Functional pKi = 7.7 7.7 - 0
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 79913 None 0 Human Functional pKi = 7.7 7.7 - 0
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 81112 None 0 Human Functional pKi = 7.7 7.7 - 0
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 81112 None 0 Human Functional pKi = 7.7 7.7 - 0
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 78231 None 0 Human Functional pKi = 6.7 6.7 - 0
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 78231 None 0 Human Functional pKi = 6.7 6.7 - 0
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 80000 None 0 Human Functional pKi = 6.7 6.7 - 0
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 80000 None 0 Human Functional pKi = 6.7 6.7 - 0
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 78138 None 0 Human Functional pKi = 8.7 8.7 - 0
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 78138 None 0 Human Functional pKi = 8.7 8.7 - 0
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 17033 None 0 Human Functional pKi = 8.7 8.7 - 0
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 17033 None 0 Human Functional pKi = 8.7 8.7 - 0
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 17036 None 0 Human Functional pKi = 8.6 8.6 - 0
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 17036 None 0 Human Functional pKi = 8.6 8.6 - 0
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 123321 None 0 Human Functional pKi = 8.6 8.6 - 0
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 123321 None 0 Human Functional pKi = 8.6 8.6 - 0
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 126020 None 0 Human Functional pKi = 8.6 8.6 - 0
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 126020 None 0 Human Functional pKi = 8.6 8.6 - 0
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 17024 None 0 Human Functional pKi = 8.6 8.6 - 0
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 17024 None 0 Human Functional pKi = 8.6 8.6 - 0
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 17046 None 0 Human Functional pKi = 8.6 8.6 - 0
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 17046 None 0 Human Functional pKi = 8.6 8.6 - 0
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 16989 None 0 Human Functional pKi = 7.7 7.7 - 0
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 16989 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17125 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17125 None 0 Human Functional pKi = 7.7 7.7 - 0
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 138288 None 0 Human Functional pKi = 7.7 7.7 - 0
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 138288 None 0 Human Functional pKi = 7.7 7.7 - 0
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 138778 None 0 Human Functional pKi = 7.7 7.7 - 1
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 138778 None 0 Human Functional pKi = 7.7 7.7 - 1
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 81154 None 0 Human Functional pKi = 7.7 7.7 - 1
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 81154 None 0 Human Functional pKi = 7.7 7.7 - 1
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 17000 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17000 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17127 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17127 None 0 Human Functional pKi = 7.7 7.7 - 0
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 72423 None 0 Human Functional pKi = 7.7 7.7 - 0
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 72423 None 0 Human Functional pKi = 7.7 7.7 - 0
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 78230 None 0 Human Functional pKi = 7.7 7.7 - 0
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 78230 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17070 None 0 Human Functional pKi = 7.7 7.7 - 0
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 17070 None 0 Human Functional pKi = 7.7 7.7 - 0
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 73988 None 0 Human Functional pKi = 6.7 6.7 - 0
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 73988 None 0 Human Functional pKi = 6.7 6.7 - 0
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 77764 None 0 Human Functional pKi = 5.7 5.7 - 0
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 77764 None 0 Human Functional pKi = 5.7 5.7 - 0
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 89358 None 0 Human Functional pKi = 7.7 7.7 - 0
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 89358 None 0 Human Functional pKi = 7.7 7.7 - 0
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 79761 None 0 Human Functional pKi = 7.7 7.7 - 0
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 79761 None 0 Human Functional pKi = 7.7 7.7 - 0
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 157805 None 0 Human Functional pKi = 7.7 7.7 - 0
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 157805 None 0 Human Functional pKi = 7.7 7.7 - 0
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 139358 None 0 Human Functional pKi = 6.7 6.7 - 0
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 139358 None 0 Human Functional pKi = 6.7 6.7 - 0
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 81608 None 0 Human Functional pKi = 6.6 6.6 - 0
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 81608 None 0 Human Functional pKi = 6.6 6.6 - 0
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 72512 None 0 Human Functional pKi = 7.6 7.6 - 0
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 72512 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138953 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138953 None 0 Human Functional pKi = 7.6 7.6 - 0
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 81616 None 0 Human Functional pKi = 7.6 7.6 - 0
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 81616 None 0 Human Functional pKi = 7.6 7.6 - 0
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 17053 None 0 Human Functional pKi = 7.6 7.6 - 0
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 17053 None 0 Human Functional pKi = 7.6 7.6 - 0
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 80408 None 0 Human Functional pKi = 7.6 7.6 - 1
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 80408 None 0 Human Functional pKi = 7.6 7.6 - 1
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 139768 None 0 Human Functional pKi = 6.6 6.6 - 0
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 139768 None 0 Human Functional pKi = 6.6 6.6 - 0
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 81568 None 0 Human Functional pKi = 5.6 5.6 - 0
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 81568 None 0 Human Functional pKi = 5.6 5.6 - 0
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 141597 None 0 Human Functional pKi = 5.6 5.6 - 0
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 141597 None 0 Human Functional pKi = 5.6 5.6 - 0
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 77784 None 0 Human Functional pKi = 6.6 6.6 - 0
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 77784 None 0 Human Functional pKi = 6.6 6.6 - 0
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 77782 None 0 Human Functional pKi = 7.6 7.6 - 0
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 77782 None 0 Human Functional pKi = 7.6 7.6 - 0
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 16982 None 0 Human Functional pKi = 7.6 7.6 - 0
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 16982 None 0 Human Functional pKi = 7.6 7.6 - 0
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 77304 None 0 Human Functional pKi = 7.6 7.6 - 0
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 77304 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138780 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138780 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138995 None 0 Human Functional pKi = 7.6 7.6 - 0
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 138995 None 0 Human Functional pKi = 7.6 7.6 - 0
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 17006 None 0 Human Functional pKi = 7.6 7.6 - 0
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 17006 None 0 Human Functional pKi = 7.6 7.6 - 0
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 71842 None 0 Human Functional pKi = 7.6 7.6 - 0
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 71842 None 0 Human Functional pKi = 7.6 7.6 - 0
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 17126 None 0 Human Functional pKi = 7.5 7.5 - 0
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 17126 None 0 Human Functional pKi = 7.5 7.5 - 0
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 78335 None 0 Human Functional pKi = 6.6 6.6 - 0
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 78335 None 0 Human Functional pKi = 6.6 6.6 - 0
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 136079 None 0 Human Functional pKi = 6.5 6.5 - 0
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 136079 None 0 Human Functional pKi = 6.5 6.5 - 0
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 17008 None 0 Human Functional pKi = 6.5 6.5 - 0
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 17008 None 0 Human Functional pKi = 6.5 6.5 - 0
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 188939 None 0 Human Functional pKi = 8.5 8.5 - 0
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 188939 None 0 Human Functional pKi = 8.5 8.5 - 0
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 78052 None 0 Human Functional pKi = 8.5 8.5 - 0
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 78052 None 0 Human Functional pKi = 8.5 8.5 - 0
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 78305 None 0 Human Functional pKi = 8.5 8.5 - 0
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 78305 None 0 Human Functional pKi = 8.5 8.5 - 0
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 79869 None 0 Human Functional pKi = 8.5 8.5 - 0
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 79869 None 0 Human Functional pKi = 8.5 8.5 - 0
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 178937 None 0 Human Functional pKi = 8.5 8.5 - 0
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 178937 None 0 Human Functional pKi = 8.5 8.5 - 0
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 189465 None 0 Human Functional pKi = 8.5 8.5 - 0
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 189465 None 0 Human Functional pKi = 8.5 8.5 - 0
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 141571 None 0 Human Functional pKi = 8.5 8.5 - 0
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 141571 None 0 Human Functional pKi = 8.5 8.5 - 0
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 17028 None 0 Human Functional pKi = 8.5 8.5 - 0
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 17028 None 0 Human Functional pKi = 8.5 8.5 - 0
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 77798 None 0 Human Functional pKi = 8.5 8.5 - 1
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 77798 None 0 Human Functional pKi = 8.5 8.5 - 1
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 78086 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78086 None 0 Human Functional pKi = 8.4 8.4 - 0
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 135324 None 0 Human Functional pKi = 8.4 8.4 - 0
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 135324 None 0 Human Functional pKi = 8.4 8.4 - 0
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 79768 None 0 Human Functional pKi = 8.4 8.4 - 0
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 79768 None 0 Human Functional pKi = 8.4 8.4 - 0
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 140243 None 0 Human Functional pKi = 7.5 7.5 - 0
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 140243 None 0 Human Functional