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Assay Detail

CHEMBL660400

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

ADMET
Inhibition of cytochrome P450 2C9
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors.
Nakamura T, Kakinuma H, Umemiya H, Amada H, Miyata N, Taniguchi K, Bando K, Sato M.
Bioorg Med Chem Lett (2004) 14 : 333 -336
PubMed 14698153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.95 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112532 1 7.02
CHEMBL113227 1 7.00
CHEMBL115876 1 6.89
CHEMBL112592 1 6.89
CHEMBL262968 1 6.73
CHEMBL114555 1 5.84
CHEMBL113018 1 5.74
CHEMBL114297 1 4.48
CHEMBL113275 1 4.48
CHEMBL325429 1 4.40
CHEMBL320105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112532 IC50 = 96.0 nM 7.02
CHEMBL113227 IC50 = 101.0 nM 7.00
CHEMBL115876 IC50 = 129.0 nM 6.89
CHEMBL112592 IC50 = 130.0 nM 6.89
CHEMBL262968 IC50 = 185.0 nM 6.73
CHEMBL114555 IC50 = 1440.0 nM 5.84
CHEMBL113018 IC50 = 1810.0 nM 5.74
CHEMBL114297 IC50 = 32800.0 nM 4.48
CHEMBL113275 IC50 = 33200.0 nM 4.48
CHEMBL325429 IC50 = 40000.0 nM 4.40
CHEMBL320105 IC50 > 100000.0 nM -