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Assay Detail

CHEMBL873905

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

Binding
In vitro inhibition of DHT production in Hs 68 (human genital fibroblast) cells.
20
Total Activities
20
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 1 (CHEMBL1787)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
Jones CD, Audia JE, Lawhorn DE, McQuaid LA, Neubauer BL, Pike AJ, Pennington PA, Stamm NB, Toomey RE, Hirsch KS.
J Med Chem (1993) 36 : 421 -423
PubMed 8381185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.51 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24955 BEXLOSTERIDE 2.0 1 8.10
CHEMBL134357 1 7.96
CHEMBL29166 1 7.77
CHEMBL16456 1 7.52
CHEMBL424084 1 7.46
CHEMBL281204 1 7.39
CHEMBL134810 1 7.22
CHEMBL335919 1 6.92
CHEMBL135014 1 6.92
CHEMBL131803 1 6.50
CHEMBL277664 1 6.34
CHEMBL57789 1 6.25
CHEMBL134114 1 6.22
CHEMBL336854 1 5.75
CHEMBL132086 1 5.64
CHEMBL441287 1 5.50
CHEMBL134819 1 5.44
CHEMBL27549 1 5.19
CHEMBL138225 EPRISTERIDE 2.0 1 5.12
CHEMBL336200 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24955 BEXLOSTERIDE IC50 = 8.0 nM 8.10
CHEMBL134357 IC50 = 11.0 nM 7.96
CHEMBL29166 IC50 = 17.0 nM 7.77
CHEMBL16456 IC50 = 30.0 nM 7.52
CHEMBL424084 IC50 = 35.0 nM 7.46
CHEMBL281204 IC50 = 41.0 nM 7.39
CHEMBL134810 IC50 = 60.0 nM 7.22
CHEMBL335919 IC50 = 120.0 nM 6.92
CHEMBL135014 IC50 = 120.0 nM 6.92
CHEMBL131803 IC50 = 320.0 nM 6.50
CHEMBL277664 IC50 = 460.0 nM 6.34
CHEMBL57789 IC50 = 560.0 nM 6.25
CHEMBL134114 IC50 = 600.0 nM 6.22
CHEMBL336854 IC50 = 1800.0 nM 5.75
CHEMBL132086 IC50 = 2300.0 nM 5.64
CHEMBL441287 IC50 = 3200.0 nM 5.50
CHEMBL134819 IC50 = 3600.0 nM 5.44
CHEMBL27549 IC50 = 6500.0 nM 5.19
CHEMBL138225 EPRISTERIDE IC50 = 7500.0 nM 5.12
CHEMBL336200 IC50 = 10000.0 nM 5.00