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Assay Detail

CHEMBL2421744

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

Binding
Inhibition of human CYP17 expressed in Escherichia coli using 1,2[3H]-progesterone as substrate in presence of NADPH
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.
Pinto-Bazurco Mendieta MA, Hu Q, Engel M, Hartmann RW.
J Med Chem (2013) 56 : 6101 -6107
PubMed 23859149 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.72 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2420683 1 7.96
CHEMBL2420684 1 7.80
CHEMBL2420674 1 7.19
CHEMBL254328 ABIRATERONE 3.0 1 7.14
CHEMBL2420681 1 7.03
CHEMBL2420675 1 6.97
CHEMBL2420677 1 6.83
CHEMBL2420682 1 6.73
CHEMBL2420687 1 6.53
CHEMBL2420678 1 6.43
CHEMBL2420679 1 6.34
CHEMBL2420680 1 6.28
CHEMBL2420676 1 6.28
CHEMBL2420685 1 6.20
CHEMBL2420688 1 5.99
CHEMBL2420686 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2420683 IC50 = 11.0 nM 7.96
CHEMBL2420684 IC50 = 16.0 nM 7.80
CHEMBL2420674 IC50 = 64.0 nM 7.19
CHEMBL254328 ABIRATERONE IC50 = 72.0 nM 7.14
CHEMBL2420681 IC50 = 94.0 nM 7.03
CHEMBL2420675 IC50 = 106.0 nM 6.97
CHEMBL2420677 IC50 = 147.0 nM 6.83
CHEMBL2420682 IC50 = 185.0 nM 6.73
CHEMBL2420687 IC50 = 294.0 nM 6.53
CHEMBL2420678 IC50 = 375.0 nM 6.43
CHEMBL2420679 IC50 = 454.0 nM 6.34
CHEMBL2420680 IC50 = 525.0 nM 6.28
CHEMBL2420676 IC50 = 523.0 nM 6.28
CHEMBL2420685 IC50 = 632.0 nM 6.20
CHEMBL2420688 IC50 = 1028.0 nM 5.99
CHEMBL2420686 IC50 = 1520.0 nM 5.82