Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL900201

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

ADMET
Inhibition of CYP2C9 in human liver microsomes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
J Med Chem (2007) 50 : 6303 -6306
PubMed 17994679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.20 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235952 1 5.80
CHEMBL236162 1 5.55
CHEMBL237247 1 5.38
CHEMBL237037 1 5.24
CHEMBL236163 1 4.82
CHEMBL237248 1 4.38
CHEMBL235256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235952 IC50 = 1600.0 nM 5.80
CHEMBL236162 IC50 = 2800.0 nM 5.55
CHEMBL237247 IC50 = 4200.0 nM 5.38
CHEMBL237037 IC50 = 5700.0 nM 5.24
CHEMBL236163 IC50 = 15000.0 nM 4.82
CHEMBL237248 IC50 = 42000.0 nM 4.38
CHEMBL235256 IC50 < 400.0 nM -