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Assay Detail

CHEMBL969605

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
18
Total Activities
17
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 spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
Suzuki T, Moriya M, Sakamoto T, Suga T, Kishino H, Takahashi H, Ishikawa M, Nagai K, Imai Y, Sekino E, Ito M, Iwaasa H, Ishihara A, Tokita S, Kanatani A, Sato N, Fukami T.
Bioorg Med Chem Lett (2009) 19 : 3072 -3077
PubMed 19403308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.43 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468099 1 10.05
CHEMBL511542 1 9.82
CHEMBL466425 2 9.34
CHEMBL494016 1 9.00
CHEMBL493962 1 8.77
CHEMBL493967 1 8.72
CHEMBL494009 1 8.68
CHEMBL522037 1 8.68
CHEMBL511747 1 8.57
CHEMBL494155 1 8.54
CHEMBL523882 1 8.02
CHEMBL494156 1 8.00
CHEMBL523697 1 7.72
CHEMBL468299 1 7.38
CHEMBL468509 1 7.38
CHEMBL468298 1 7.27
CHEMBL467668 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468099 IC50 = 0.09 nM 10.05
CHEMBL511542 IC50 = 0.15 nM 9.82
CHEMBL466425 IC50 = 0.46 nM 9.34
CHEMBL494016 IC50 = 1.0 nM 9.00
CHEMBL466425 IC50 = 1.3 nM 8.89
CHEMBL493962 IC50 = 1.7 nM 8.77
CHEMBL493967 IC50 = 1.9 nM 8.72
CHEMBL494009 IC50 = 2.1 nM 8.68
CHEMBL522037 IC50 = 2.1 nM 8.68
CHEMBL511747 IC50 = 2.7 nM 8.57
CHEMBL494155 IC50 = 2.9 nM 8.54
CHEMBL523882 IC50 = 9.6 nM 8.02
CHEMBL494156 IC50 = 9.9 nM 8.00
CHEMBL523697 IC50 = 19.0 nM 7.72
CHEMBL468299 IC50 = 42.0 nM 7.38
CHEMBL468509 IC50 = 42.0 nM 7.38
CHEMBL468298 IC50 = 54.0 nM 7.27
CHEMBL467668 IC50 = 125.0 nM 6.90