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Assay Detail

CHEMBL889923

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

ADMET
Inhibition of human CYP2C9
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.
Giblin GM, Bit RA, Brown SH, Chaignot HM, Chowdhury A, Chessell IP, Clayton NM, Coleman T, Hall A, Hammond B, Hurst DN, Michel AD, Naylor A, Novelli R, Scoccitti T, Spalding D, Tang SP, Wilson AW, Wilson R.
Bioorg Med Chem Lett (2007) 17 : 385 -389
PubMed 17084082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.04 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395542 1 5.30
CHEMBL233245 1 5.27
CHEMBL389796 1 5.05
CHEMBL389996 1 4.92
CHEMBL234940 1 4.85
CHEMBL233043 1 4.85
CHEMBL234290 1 -
CHEMBL234939 1 -
CHEMBL389994 1 -
CHEMBL233044 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395542 IC50 = 5000.0 nM 5.30
CHEMBL233245 IC50 = 5400.0 nM 5.27
CHEMBL389796 IC50 = 9000.0 nM 5.05
CHEMBL389996 IC50 = 12000.0 nM 4.92
CHEMBL234940 IC50 = 14000.0 nM 4.85
CHEMBL233043 IC50 = 14000.0 nM 4.85
CHEMBL234290 IC50 - -
CHEMBL234939 IC50 - -
CHEMBL389994 IC50 - -
CHEMBL233044 IC50 - -