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Assay Detail

CHEMBL4256957

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

Binding
Inhibition of human membrane bound C-terminal His4-tagged CYP17A1 delta19H mutant assessed as reduction in progesterone hydroxylation preincubated for 3 mins followed by NADPH addition measured after 10 mins in presence of NADPH-cytochrome p450 reductase by HPLC method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of cyp17a1
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.35 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4210141 1 6.92
CHEMBL254328 ABIRATERONE 3.0 1 6.89
CHEMBL4280255 1 6.82
CHEMBL4209941 1 6.76
CHEMBL4293668 1 6.74
CHEMBL4289220 1 6.70
CHEMBL4209916 1 6.68
CHEMBL4279184 1 6.61
CHEMBL2105738 GALETERONE 3.0 1 6.55
CHEMBL4294403 1 6.37
CHEMBL4276910 1 5.86
CHEMBL4288206 1 5.40
CHEMBL1921976 ORTERONEL 3.0 1 5.33
CHEMBL4210952 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4210141 IC50 = 120.0 nM 6.92
CHEMBL254328 ABIRATERONE IC50 = 130.0 nM 6.89
CHEMBL4280255 IC50 = 150.0 nM 6.82
CHEMBL4209941 IC50 = 174.0 nM 6.76
CHEMBL4293668 IC50 = 183.0 nM 6.74
CHEMBL4289220 IC50 = 199.0 nM 6.70
CHEMBL4209916 IC50 = 208.0 nM 6.68
CHEMBL4279184 IC50 = 244.0 nM 6.61
CHEMBL2105738 GALETERONE IC50 = 282.0 nM 6.55
CHEMBL4294403 IC50 = 428.0 nM 6.37
CHEMBL4276910 IC50 = 1380.0 nM 5.86
CHEMBL4288206 IC50 = 3970.0 nM 5.40
CHEMBL1921976 ORTERONEL IC50 = 4730.0 nM 5.33
CHEMBL4210952 IC50 = 5410.0 nM 5.27