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Assay Detail

CHEMBL1293108

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

ADMET
Inhibition of CYP3A4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.
Hadden M, Deering DM, Henderson AJ, Surman MD, Luche M, Khmelnitsky Y, Vickers S, Viggers J, Cheetham S, Guzzo PR.
Bioorg Med Chem Lett (2010) 20 : 7020 -7023
PubMed 20951036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.76 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214957 1 5.80
CHEMBL1290150 1 5.77
CHEMBL1290041 1 5.70
CHEMBL1289614 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214957 IC50 = 1600.0 nM 5.80
CHEMBL1290150 IC50 = 1700.0 nM 5.77
CHEMBL1290041 IC50 = 2000.0 nM 5.70
CHEMBL1289614 IC50 < 50.0 nM -