Ligand source activities (1 row/activity)
| 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
| |
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
| |
| 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 | ||
Showing 1 to 50 of 77 entries
| 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
| |
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 | ||
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