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Assay Detail

CHEMBL1039121

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

Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cells
15
Total Activities
15
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 Intermediate

Target

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

Publication

Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.
Suzuki T, Kameda M, Ando M, Miyazoe H, Sekino E, Ito S, Masutani K, Kamijo K, Takezawa A, Moriya M, Ito M, Ito J, Nakase K, Matsushita H, Ishihara A, Takenaga N, Tokita S, Kanatani A, Sato N, Fukami T.
Bioorg Med Chem Lett (2009) 19 : 5339 -5345
PubMed 19683441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.93 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468099 1 10.05
CHEMBL568571 1 9.92
CHEMBL566880 1 9.66
CHEMBL582978 1 9.59
CHEMBL582792 1 9.46
CHEMBL538425 1 9.44
CHEMBL565614 1 8.92
CHEMBL585856 1 8.89
CHEMBL566257 1 8.85
CHEMBL568361 1 8.59
CHEMBL593521 1 8.46
CHEMBL585509 1 8.34
CHEMBL568572 1 8.20
CHEMBL585664 1 8.17
CHEMBL585880 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468099 IC50 = 0.09 nM 10.05
CHEMBL568571 IC50 = 0.12 nM 9.92
CHEMBL566880 IC50 = 0.22 nM 9.66
CHEMBL582978 IC50 = 0.26 nM 9.59
CHEMBL582792 IC50 = 0.35 nM 9.46
CHEMBL538425 IC50 = 0.36 nM 9.44
CHEMBL565614 IC50 = 1.2 nM 8.92
CHEMBL585856 IC50 = 1.3 nM 8.89
CHEMBL566257 IC50 = 1.4 nM 8.85
CHEMBL568361 IC50 = 2.6 nM 8.59
CHEMBL593521 IC50 = 3.5 nM 8.46
CHEMBL585509 IC50 = 4.6 nM 8.34
CHEMBL568572 IC50 = 6.3 nM 8.20
CHEMBL585664 IC50 = 6.8 nM 8.17
CHEMBL585880 IC50 = 45.0 nM 7.35