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Assay Detail

CHEMBL3856907

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

Binding
Inhibition of Wistar rat testicular C17,20-lyase assessed as androst-4-ene-3,17-dione formation using [3H]17-hydroxyprogesterone as substrate in presence of NADPH
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL4430)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of novel 17-(4'-formyl)pyrazolylandrosta-5,16-dienes and their derivatives as potent 17α-hydroxylase/C17,20-lyase inhibitors or antiproliferative agents depending on the substitution pattern of the heteroring.
Kovács D, Wölfling J, Szabó N, Szécsi M, Schelz Z, Zupkó I, Frank É.
Eur J Med Chem (2016) 120 : 284 -295
PubMed 27209562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.39 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112517 1 8.11
CHEMBL254328 ABIRATERONE 3.0 1 7.90
CHEMBL3966872 1 7.58
CHEMBL3912227 1 7.18
CHEMBL3947033 1 7.04
CHEMBL157101 KETOCONAZOLE 4.0 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112517 IC50 = 7.7 nM 8.11
CHEMBL254328 ABIRATERONE IC50 = 12.5 nM 7.90
CHEMBL3966872 IC50 = 26.0 nM 7.58
CHEMBL3912227 IC50 = 66.0 nM 7.18
CHEMBL3947033 IC50 = 92.0 nM 7.04
CHEMBL157101 KETOCONAZOLE IC50 = 320.0 nM 6.50