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Assay Detail

CHEMBL4256958

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

ADMET
Inhibition of human membrane bound C-terminal His4-tagged CYP21A2 delta19H mutant assessed as reduction in progesterone hydroxylation measured after 10 mins in presence of NADPH/NADPH-cytochrome p450 reductase by GC/MS method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Steroid 21-hydroxylase (CHEMBL2759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of cyp17a1
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.84 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105738 GALETERONE 3.0 1 6.61
CHEMBL254328 ABIRATERONE 3.0 1 6.53
CHEMBL4209941 1 6.27
CHEMBL4209916 1 6.08
CHEMBL1921976 ORTERONEL 3.0 1 5.31
CHEMBL4210141 1 5.06
CHEMBL4280255 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105738 GALETERONE IC50 = 248.0 nM 6.61
CHEMBL254328 ABIRATERONE IC50 = 296.0 nM 6.53
CHEMBL4209941 IC50 = 537.0 nM 6.27
CHEMBL4209916 IC50 = 831.0 nM 6.08
CHEMBL1921976 ORTERONEL IC50 = 4870.0 nM 5.31
CHEMBL4210141 IC50 = 8700.0 nM 5.06
CHEMBL4280255 IC50 = 10300.0 nM 4.99