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Assay Detail

CHEMBL870679

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

ADMET
Inhibition of CYP450 2C9
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
Hall A, Bit RA, Brown SH, Chaignot HM, Chessell IP, Coleman T, Giblin GM, Hurst DN, Kilford IR, Lewell XQ, Michel AD, Mohamed S, Naylor A, Novelli R, Skinner L, Spalding DJ, Tang SP, Wilson RJ.
Bioorg Med Chem Lett (2006) 16 : 2666 -2671
PubMed 16503138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.32 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207293 1 5.72
CHEMBL207174 1 5.41
CHEMBL209244 1 5.37
CHEMBL207577 1 5.24
CHEMBL377852 1 5.19
CHEMBL377649 1 5.17
CHEMBL383090 1 5.14
CHEMBL206096 1 -
CHEMBL207688 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207293 IC50 = 1900.0 nM 5.72
CHEMBL207174 IC50 = 3900.0 nM 5.41
CHEMBL209244 IC50 = 4300.0 nM 5.37
CHEMBL207577 IC50 = 5700.0 nM 5.24
CHEMBL377852 IC50 = 6500.0 nM 5.19
CHEMBL377649 IC50 = 6800.0 nM 5.17
CHEMBL383090 IC50 = 7300.0 nM 5.14
CHEMBL206096 IC50 > 50000.0 nM -
CHEMBL207688 IC50 - -