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Assay Detail

CHEMBL809545

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

Binding
Evaluated for the inhibitory activity against human steroid 5-alpha-reductase type 2 from human BPH tissue at 210 nM of testosterone
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
Hartmann RW, Hector M, Haidar S, Ehmer PB, Reichert W, Jose J.
J Med Chem (2000) 43 : 4266 -4277
PubMed 11063622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.47 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL710 FINASTERIDE 4.0 1 8.52
CHEMBL135993 1 6.52
CHEMBL136097 1 6.37
CHEMBL2112735 1 6.37
CHEMBL137040 1 6.33
CHEMBL135651 2 6.24
CHEMBL344363 1 5.50
CHEMBL135351 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL710 FINASTERIDE IC50 = 3.0 nM 8.52
CHEMBL135993 IC50 = 300.0 nM 6.52
CHEMBL136097 IC50 = 430.0 nM 6.37
CHEMBL2112735 IC50 = 430.0 nM 6.37
CHEMBL137040 IC50 = 470.0 nM 6.33
CHEMBL135651 IC50 = 580.0 nM 6.24
CHEMBL135651 IC50 = 1170.0 nM 5.93
CHEMBL344363 IC50 = 3200.0 nM 5.50
CHEMBL135351 IC50 > 10000.0 nM -