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Assay Detail

CHEMBL3373987

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

Binding
Inhibition of human prostate 5alpha-reductase type 2 assessed as conversion of [3H]testosterone to dihydrotestosterone
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3-oxo-5-alpha-steroid 4-dehydrogenase 2 (CHEMBL1856)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
Bratoeff E, Garrido M, Ramírez-Apan T, Heuze Y, Sánchez A, Soriano J, Cabeza M.
Bioorg Med Chem (2014) 22 : 6233 -6241
PubMed 25261928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.85 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342891 1 8.49
CHEMBL3342894 1 8.10
CHEMBL710 FINASTERIDE 4.0 1 8.07
CHEMBL3342892 1 7.89
CHEMBL3342895 1 7.82
CHEMBL3342896 1 7.30
CHEMBL3342893 1 7.30
CHEMBL157101 KETOCONAZOLE 4.0 1 -
CHEMBL3342906 1 -
CHEMBL3342905 1 -
CHEMBL3342904 1 -
CHEMBL3342903 1 -
CHEMBL3342902 1 -
CHEMBL3342901 1 -
CHEMBL3342900 1 -
CHEMBL3342899 1 -
CHEMBL3342898 1 -
CHEMBL3342897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342891 IC50 = 3.2 nM 8.49
CHEMBL3342894 IC50 = 8.0 nM 8.10
CHEMBL710 FINASTERIDE IC50 = 8.5 nM 8.07
CHEMBL3342892 IC50 = 13.0 nM 7.89
CHEMBL3342895 IC50 = 15.0 nM 7.82
CHEMBL3342896 IC50 = 50.0 nM 7.30
CHEMBL3342893 IC50 = 50.0 nM 7.30
CHEMBL157101 KETOCONAZOLE IC50 - -
CHEMBL3342906 IC50 - -
CHEMBL3342905 IC50 - -
CHEMBL3342904 IC50 - -
CHEMBL3342903 IC50 - -
CHEMBL3342902 IC50 - -
CHEMBL3342901 IC50 - -
CHEMBL3342900 IC50 - -
CHEMBL3342899 IC50 - -
CHEMBL3342898 IC50 - -
CHEMBL3342897 IC50 - -