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Assay Detail

CHEMBL662841

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

Binding
Binding affinity for Cytochrome P450 17A1 (17-alpha-hydroxypregnenolone Km=560 nM)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.
Njar VC, Kato K, Nnane IP, Grigoryev DN, Long BJ, Brodie AM.
J Med Chem (1998) 41 : 902 -912
PubMed 9526564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.16 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74661 1 8.92
CHEMBL78108 1 8.85
CHEMBL310336 1 8.72
CHEMBL310822 1 7.64
CHEMBL157101 KETOCONAZOLE 4.0 1 7.42
CHEMBL307729 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74661 Ki = 1.2 nM 8.92
CHEMBL78108 Ki = 1.4 nM 8.85
CHEMBL310336 Ki = 1.9 nM 8.72
CHEMBL310822 Ki = 23.0 nM 7.64
CHEMBL157101 KETOCONAZOLE Ki = 38.0 nM 7.42
CHEMBL307729 Ki = 41.0 nM 7.39