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Assay Detail

CHEMBL5224657

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ADMET
Inhibition of recombinant human CYP3A4
1
Total Activities
1
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 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Padmakar Darne C, Velaparthi U, Saulnier M, Frennesson D, Liu P, Huang A, Tokarski J, Fura A, Spires T, Newitt J, Spires VM, Obermeier MT, Elzinga PA, Gottardis MM, Jayaraman L, Vite GD, Balog A.
Bioorg Med Chem Lett (2022) 75 : 128951 -128951
PubMed 36031020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.44 4.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5290029 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5290029 IC50 = 36000.0 nM 4.44