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Assay Detail

CHEMBL812008

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

Binding
Inhibition of Steroid 5-alpha-reductase type I from rat ventral prostate (RVP)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Prostate gland
Confidence 9 — Direct single protein target
Curated By Expert

Target

3-oxo-5-alpha-steroid 4-dehydrogenase 1 (CHEMBL3422)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.
Picard F, Barassin S, Mokhtarian A, Hartmann RW.
J Med Chem (2002) 45 : 3406 -3417
PubMed 12139451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.89 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL710 FINASTERIDE 4.0 1 8.00
CHEMBL114594 1 6.27
CHEMBL117881 1 5.96
CHEMBL117643 1 5.80
CHEMBL116621 1 5.72
CHEMBL115123 1 5.57
CHEMBL115438 1 5.50
CHEMBL115298 1 5.47
CHEMBL323856 1 5.35
CHEMBL114114 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL710 FINASTERIDE IC50 = 10.0 nM 8.00
CHEMBL114594 IC50 = 540.0 nM 6.27
CHEMBL117881 IC50 = 1100.0 nM 5.96
CHEMBL117643 IC50 = 1600.0 nM 5.80
CHEMBL116621 IC50 = 1900.0 nM 5.72
CHEMBL115123 IC50 = 2700.0 nM 5.57
CHEMBL115438 IC50 = 3200.0 nM 5.50
CHEMBL115298 IC50 = 3400.0 nM 5.47
CHEMBL323856 IC50 = 4500.0 nM 5.35
CHEMBL114114 IC50 = 5600.0 nM 5.25