Ligand source activities (1 row/activity)



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

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
57401968 69545 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 69545 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 69547 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 69547 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 69551 0 None 501 2 Human 9.0 pIC50 = 9 Functional
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 69551 0 None 501 2 Human 9.0 pIC50 = 9 Functional
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 69554 0 None 1513 2 Human 9.0 pIC50 = 9 Functional
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 69554 0 None 1513 2 Human 9.0 pIC50 = 9 Functional
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 69540 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69540 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69550 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69550 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69552 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69552 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69531 1 None - 1 Human 7.0 pIC50 = 7 Functional
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 69531 1 None - 1 Human 7.0 pIC50 = 7 Functional
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 69537 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 69537 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 69543 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 69543 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 69526 4 None 19 2 Human 6.0 pIC50 = 6 Functional
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 69526 4 None 19 2 Human 6.0 pIC50 = 6 Functional
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 69527 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 69527 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 69546 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 69546 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 69542 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 69542 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 69528 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
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 69528 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
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 69535 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 69535 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 69539 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 69539 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 69544 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 69544 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 69548 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 69548 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 69538 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 69538 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 69534 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 69534 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 69533 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 69533 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 69536 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 69536 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 69529 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 69529 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 69530 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 69530 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 69553 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 69553 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 69532 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 69532 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 69549 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 69549 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 69541 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 69541 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 0 None - 1 Human 5.9 pIC50 None 5.9 Functional
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 0 None - 1 Human 5.9 pIC50 None 5.9 Functional
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 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
101600353 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
1301 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1301 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
134824567 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
134824567 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
16207764 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
16207764 2470 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838
1307 528 0 None 1 2 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1290 258 0 None -15 2 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1298 2484 0 None - 1 Human 8.7 pIC50 None 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
16167454 2484 0 None - 1 Human 8.7 pIC50 None 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
91898993 2484 0 None - 1 Human 8.7 pIC50 None 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1297 3103 0 None -1 2 Human 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
1297 3103 0 None -1 2 Human 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11459838


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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selectivity		 # Tested
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 p-value
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Type		 Assay
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 DOI
9806086 65207 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 65207 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 66206 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 66206 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 66996 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 66996 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 71759 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 71759 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 70308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 70308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 71862 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 71862 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 194897 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 194897 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 71196 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 71196 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 71871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 71871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 166376 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 166376 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 66171 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 66171 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 71724 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 71724 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 71461 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 71461 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 70561 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 70561 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 82438 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 82438 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 195762 0 None -46 3 Human 8.8 pKi = 8.8 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human 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 195762 0 None -46 3 Human 8.8 pKi = 8.8 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human 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 195762 0 None -46 3 Human 8.8 pKi = 8.8 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human 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 69554 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 69554 0 None - 1 Human 7.9 pKi = 7.9 Binding
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