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Assay Detail

CHEMBL760886

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

Binding
Inhibition of human progesterone 17-alpha-hydroxylase.
9
Total Activities
9
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

The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors.
Jarman M, Barrie SE, Llera JM.
J Med Chem (1998) 41 : 5375 -5381
PubMed 9876107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.61 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432751 1 8.52
CHEMBL254328 ABIRATERONE 3.0 1 8.40
CHEMBL3137967 1 8.30
CHEMBL310315 1 7.89
CHEMBL357811 1 7.57
CHEMBL82926 1 7.33
CHEMBL3137965 1 7.13
CHEMBL310690 1 6.80
CHEMBL2112888 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432751 IC50 = 3.0 nM 8.52
CHEMBL254328 ABIRATERONE IC50 = 4.0 nM 8.40
CHEMBL3137967 IC50 = 5.0 nM 8.30
CHEMBL310315 IC50 = 13.0 nM 7.89
CHEMBL357811 IC50 = 27.0 nM 7.57
CHEMBL82926 IC50 = 47.0 nM 7.33
CHEMBL3137965 IC50 = 74.0 nM 7.13
CHEMBL310690 IC50 = 160.0 nM 6.80
CHEMBL2112888 IC50 = 260.0 nM 6.58