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

 Mol
weight		 Rot
Bonds		 H don

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 DOI
57401968 69567 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 451 4 1 3 5.9 CCn1c2ccccc2c2cc(CN3CCC4(CC3)CC(NC(C)=O)c3ccccc34)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934121 69567 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 451 4 1 3 5.9 CCn1c2ccccc2c2cc(CN3CCC4(CC3)CC(NC(C)=O)c3ccccc34)ccc21 10.1016/j.bmcl.2011.10.125
10410064 69569 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 423 3 2 2 5.4 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934123 69569 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 423 3 2 2 5.4 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
57394992 69573 None 0 Human Functional pIC50 = 9 9.0 501 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 457 3 2 2 6.1 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(Cl)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934127 69573 None 0 Human Functional pIC50 = 9 9.0 501 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 457 3 2 2 6.1 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(Cl)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
10457264 69576 None 0 Human Functional pIC50 = 9 9.0 1513 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 466 3 2 4 4.8 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4c(c3)c3ccccc3n4C(N)=O)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934130 69576 None 0 Human Functional pIC50 = 9 9.0 1513 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 466 3 2 4 4.8 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4c(c3)c3ccccc3n4C(N)=O)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
10091316 69562 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 382 2 2 2 4.8 O[C@@H]1Cc2ccccc2C12CCN(Cc1ccc3[nH]c4ccccc4c3c1)CC2 10.1016/j.bmcl.2011.10.125
CHEMBL1934116 69562 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 382 2 2 2 4.8 O[C@@H]1Cc2ccccc2C12CCN(Cc1ccc3[nH]c4ccccc4c3c1)CC2 10.1016/j.bmcl.2011.10.125
57391501 69572 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 441 3 2 2 5.6 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(F)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934126 69572 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 441 3 2 2 5.6 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(F)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
57396735 69574 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 501 3 2 2 6.2 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(Br)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934128 69574 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 501 3 2 2 6.2 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(Br)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
10090198 69553 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 364 2 1 1 5.9 C1=CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934107 69553 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 364 2 1 1 5.9 C1=CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
10025150 69559 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 420 3 0 3 6.4 CCC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934113 69559 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 420 3 0 3 6.4 CCC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57401967 69565 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 467 4 2 4 4.9 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](NC(C)=O)[C@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934119 69565 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 467 4 2 4 4.9 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](NC(C)=O)[C@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
30979231 69548 None 4 Human Functional pIC50 = 6 6.0 19 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation 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 = 6 6.0 19 2
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57403720 69549 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 4 0 2 6.4 CCn1c2ccccc2c2cc(CCN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934103 69549 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 4 0 2 6.4 CCn1c2ccccc2c2cc(CCN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57401969 69568 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 423 3 2 2 5.4 CC(=O)N[C@H]1CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934122 69568 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 423 3 2 2 5.4 CC(=O)N[C@H]1CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
57400179 69564 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 426 3 2 4 4.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](O)[C@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934118 69564 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 426 3 2 4 4.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](O)[C@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
57396733 69550 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 420 5 0 2 6.8 CCn1c2ccccc2c2cc(CCCN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934104 69550 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 420 5 0 2 6.8 CCn1c2ccccc2c2cc(CCCN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57396734 69557 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 442 3 0 4 5.2 CS(=O)(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934111 69557 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 442 3 0 4 5.2 CS(=O)(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57400177 69561 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 410 3 1 3 5.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)CC(O)c3ccccc34)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934115 69561 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 410 3 1 3 5.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)CC(O)c3ccccc34)ccc21 10.1016/j.bmcl.2011.10.125
57394991 69566 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 451 4 1 3 5.4 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3CC4NC(C)=O)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934120 69566 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 451 4 1 3 5.4 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3CC4NC(C)=O)ccc21 10.1016/j.bmcl.2011.10.125
57403723 69570 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 426 3 2 4 4.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](O)[C@@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934124 69570 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 426 3 2 4 4.8 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3[C@H](O)[C@@H]4O)ccc21 10.1016/j.bmcl.2011.10.125
23572819 69560 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 410 3 1 3 5.3 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3CC4O)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934114 69560 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 410 3 1 3 5.3 CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3CC4O)ccc21 10.1016/j.bmcl.2011.10.125
57400176 69556 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 422 2 0 4 6.0 COC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934110 69556 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 422 2 0 4 6.0 COC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
10455647 69555 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 435 2 0 3 5.9 CN(C)C(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934109 69555 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 435 2 0 3 5.9 CN(C)C(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
10046992 69558 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 407 2 1 3 5.3 NC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934112 69558 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 407 2 1 3 5.3 NC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57403721 69551 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 2 0 2 6.0 CCn1c2ccccc2c2cc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934105 69551 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 2 0 2 6.0 CCn1c2ccccc2c2cc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57401966 69552 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 421 2 1 2 6.4 CCn1c2ccccc2c2cc(NC(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934106 69552 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 421 2 1 2 6.4 CCn1c2ccccc2c2cc(NC(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57391502 69575 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 491 3 2 2 6.5 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(C(F)(F)F)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934129 69575 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 491 3 2 2 6.5 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4[nH]c5ccc(C(F)(F)F)cc5c4c3)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
57403722 69554 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 2 0 3 6.0 CC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934108 69554 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 406 2 0 3 6.0 CC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
57400180 69571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 439 3 3 3 4.4 CC(=O)N[C@H]1c2ccccc2C2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)[C@@H]1O 10.1016/j.bmcl.2011.10.125
CHEMBL1934125 69571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 439 3 3 3 4.4 CC(=O)N[C@H]1c2ccccc2C2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)[C@@H]1O 10.1016/j.bmcl.2011.10.125
57400178 69563 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 382 2 2 2 4.8 O[C@H]1Cc2ccccc2C12CCN(Cc1ccc3[nH]c4ccccc4c3c1)CC2 10.1016/j.bmcl.2011.10.125
CHEMBL1934117 69563 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assayAntagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay
ChEMBL 382 2 2 2 4.8 O[C@H]1Cc2ccccc2C12CCN(Cc1ccc3[nH]c4ccccc4c3c1)CC2 10.1016/j.bmcl.2011.10.125
7757 1078 None 0 Human Functional pIC50 = 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 466 5 2 4 5.7 CCCN[C@@H]1CC2(c3c1cccc3)CCN(CC2)Cc1ccc2c(c1)c1ccccc1n2C(=O)N 22123324
86277835 1078 None 0 Human Functional pIC50 = 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 466 5 2 4 5.7 CCCN[C@@H]1CC2(c3c1cccc3)CCN(CC2)Cc1ccc2c(c1)c1ccccc1n2C(=O)N 22123324
11238212 510 None 0 Human Functional pIC50 None 5.9 5.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1304 510 None 0 Human Functional pIC50 None 5.9 5.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
101600353 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
101600353 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
1301 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1301 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
134824567 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
134824567 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
16207764 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
16207764 2470 None 0 Human Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
1307 528 None 0 Human Functional pIC50 None 7.3 7.3 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1290 258 None 0 Human Functional pIC50 None 8.6 8.6 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1298 2484 None 0 Human Functional pIC50 None 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
16167454 2484 None 0 Human Functional pIC50 None 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
91898993 2484 None 0 Human Functional pIC50 None 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1297 3103 None 0 Human Functional pIC50 None 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1297 3103 None 0 Human Functional pIC50 None 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838


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

 Species

 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
9806086 65228 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 65228 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
10436090 66227 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 66227 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44395076 67017 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 67017 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
10388797 71783 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71783 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11512135 70332 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 70332 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
10027853 71886 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71886 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11599973 195697 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCH from human MCHR2 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR2 expressed in CHO cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 195697 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCH from human MCHR2 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR2 expressed in CHO cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
11548234 71220 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 71220 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11201645 71895 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71895 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44403765 135936 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135936 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
10005009 166471 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 166471 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
9955811 66192 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 66192 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
11583744 71748 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71748 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11648240 71485 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71485 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11539632 70585 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70585 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
10173787 82470 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R2Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R2
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 Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R2Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R2
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
45273336 198218 None 0 Human Binding pKi = 8.8 8.8 -46 3
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 198218 None 0 Human Binding pKi = 8.8 8.8 -46 3
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 198218 None 0 Human Binding pKi = 8.8 8.8 -46 3
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
10457264 69576 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]N-(1'-((9-ethyl-9H-carbazol-3-yl)methyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-yl)acetamide from human MCHR2 expressed in HEK293 cells after 2 hrsDisplacement of [3H]N-(1'-((9-ethyl-9H-carbazol-3-yl)methyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-yl)acetamide from human MCHR2 expressed in HEK293 cells after 2 hrs
ChEMBL 466 3 2 4 4.8 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4c(c3)c3ccccc3n4C(N)=O)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934130 69576 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]N-(1'-((9-ethyl-9H-carbazol-3-yl)methyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-yl)acetamide from human MCHR2 expressed in HEK293 cells after 2 hrsDisplacement of [3H]N-(1'-((9-ethyl-9H-carbazol-3-yl)methyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-yl)acetamide from human MCHR2 expressed in HEK293 cells after 2 hrs
ChEMBL 466 3 2 4 4.8 CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4c(c3)c3ccccc3n4C(N)=O)CC2)c2ccccc21 10.1016/j.bmcl.2011.10.125