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Assay Detail

CHEMBL1799313

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

ADMET
Reversible inhibition of CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestosterone
1
Total Activities
1
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

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S.
Bioorg Med Chem Lett (2011) 21 : 3970 -3975
PubMed 21621998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.19 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1796063 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1796063 IC50 = 6500.0 nM 5.19