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Assay Detail

CHEMBL1648561

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanin-concentrating hormone receptor 1 (CHEMBL344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
Haga Y, Mizutani S, Naya A, Kishino H, Iwaasa H, Ito M, Ito J, Moriya M, Sato N, Takenaga N, Ishihara A, Tokita S, Kanatani A, Ohtake N.
Bioorg Med Chem (2011) 19 : 883 -893
PubMed 21190859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.89 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642475 1 8.85
CHEMBL179501 1 8.85
CHEMBL1642487 1 8.42
CHEMBL1642474 1 8.38
CHEMBL1642482 1 8.36
CHEMBL1642486 1 8.29
CHEMBL178707 1 8.26
CHEMBL584538 1 8.25
CHEMBL1641614 1 8.24
CHEMBL1642472 1 8.23
CHEMBL1642485 1 8.18
CHEMBL1642492 1 8.17
CHEMBL1642477 1 8.17
CHEMBL1642476 1 8.15
CHEMBL1642479 1 8.11
CHEMBL1642471 1 8.06
CHEMBL1642484 1 8.02
CHEMBL1642491 1 7.92
CHEMBL1642473 1 7.92
CHEMBL1642493 1 7.80
CHEMBL1642490 1 7.75
CHEMBL1642470 1 7.75
CHEMBL1642468 1 7.62
CHEMBL1642488 1 7.29
CHEMBL1642469 1 6.82
CHEMBL1642489 1 6.75
CHEMBL1642483 1 6.19
CHEMBL1642478 1 6.19
CHEMBL1642494 1 -
CHEMBL1642480 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642475 IC50 = 1.4 nM 8.85
CHEMBL179501 IC50 = 1.4 nM 8.85
CHEMBL1642487 IC50 = 3.8 nM 8.42
CHEMBL1642474 IC50 = 4.2 nM 8.38
CHEMBL1642482 IC50 = 4.4 nM 8.36
CHEMBL1642486 IC50 = 5.1 nM 8.29
CHEMBL178707 IC50 = 5.5 nM 8.26
CHEMBL584538 IC50 = 5.6 nM 8.25
CHEMBL1641614 IC50 = 5.8 nM 8.24
CHEMBL1642472 IC50 = 5.9 nM 8.23
CHEMBL1642485 IC50 = 6.6 nM 8.18
CHEMBL1642492 IC50 = 6.8 nM 8.17
CHEMBL1642477 IC50 = 6.7 nM 8.17
CHEMBL1642476 IC50 = 7.0 nM 8.15
CHEMBL1642479 IC50 = 7.7 nM 8.11
CHEMBL1642471 IC50 = 8.7 nM 8.06
CHEMBL1642484 IC50 = 9.5 nM 8.02
CHEMBL1642491 IC50 = 12.0 nM 7.92
CHEMBL1642473 IC50 = 12.0 nM 7.92
CHEMBL1642493 IC50 = 16.0 nM 7.80
CHEMBL1642490 IC50 = 18.0 nM 7.75
CHEMBL1642470 IC50 = 18.0 nM 7.75
CHEMBL1642468 IC50 = 24.0 nM 7.62
CHEMBL1642488 IC50 = 51.0 nM 7.29
CHEMBL1642469 IC50 = 150.0 nM 6.82
CHEMBL1642489 IC50 = 180.0 nM 6.75
CHEMBL1642483 IC50 = 650.0 nM 6.19
CHEMBL1642478 IC50 = 640.0 nM 6.19
CHEMBL1642494 IC50 > 1000.0 nM -
CHEMBL1642480 IC50 > 1000.0 nM -
CHEMBL1642481 IC50 > 1000.0 nM -