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Assay Detail

CHEMBL811228

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

Binding
Ability to inhibit the Steroid 17-alpha-hydroxylase/17,20 lyase enzyme by 50%.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.
Potter GA, Barrie SE, Jarman M, Rowlands MG.
J Med Chem (1995) 38 : 2463 -2471
PubMed 7608911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.62 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310662 1 8.59
CHEMBL432751 1 8.55
CHEMBL254328 ABIRATERONE 3.0 1 8.40
CHEMBL79829 1 8.37
CHEMBL84230 1 8.33
CHEMBL310315 1 7.90
CHEMBL311444 1 7.89
CHEMBL271227 ABIRATERONE ACETATE 4.0 1 7.75
CHEMBL82926 1 7.33
CHEMBL157101 KETOCONAZOLE 4.0 1 7.19
CHEMBL310690 1 6.80
CHEMBL2112301 1 6.57
CHEMBL2112299 1 5.40
CHEMBL79319 1 -
CHEMBL439582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310662 IC50 = 2.6 nM 8.59
CHEMBL432751 IC50 = 2.8 nM 8.55
CHEMBL254328 ABIRATERONE IC50 = 4.0 nM 8.40
CHEMBL79829 IC50 = 4.3 nM 8.37
CHEMBL84230 IC50 = 4.7 nM 8.33
CHEMBL310315 IC50 = 12.5 nM 7.90
CHEMBL311444 IC50 = 13.0 nM 7.89
CHEMBL271227 ABIRATERONE ACETATE IC50 = 18.0 nM 7.75
CHEMBL82926 IC50 = 47.0 nM 7.33
CHEMBL157101 KETOCONAZOLE IC50 = 65.0 nM 7.19
CHEMBL310690 IC50 = 160.0 nM 6.80
CHEMBL2112301 IC50 = 270.0 nM 6.57
CHEMBL2112299 IC50 = 4000.0 nM 5.40
CHEMBL79319 IC50 > 10000.0 nM -
CHEMBL439582 IC50 > 10000.0 nM -