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Assay Detail

CHEMBL808568

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

Binding
In vitro inhibitory concentration required to inhibit Steroid 5-alpha-reductase type 1 in cultured Hs 68 human foreskin fibroblast cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Fibroblast
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

QSAR study of benzoquinolinones as inhibitors of human type 1 5--reductase.
Wikel JH, Bemis KG, Audia JE, McQuaid LA, Jones CD, Pennington PA, Lawhorn DE, Hirsch KR, Stamm NB
Bioorg Med Chem Lett (1993) 3 : 1157 -1162
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.04 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279131 1 8.10
CHEMBL279417 1 7.49
CHEMBL15917 1 7.49
CHEMBL279420 1 7.49
CHEMBL278957 1 7.46
CHEMBL278981 1 7.46
CHEMBL16494 1 7.22
CHEMBL439910 1 7.10
CHEMBL439908 1 7.05
CHEMBL16027 1 6.94
CHEMBL16330 1 6.94
CHEMBL16152 1 6.82
CHEMBL16456 1 6.76
CHEMBL277091 1 6.25
CHEMBL278049 1 6.00
CHEMBL16248 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279131 IC50 = 7.943 nM 8.10
CHEMBL279417 IC50 = 32.36 nM 7.49
CHEMBL15917 IC50 = 32.36 nM 7.49
CHEMBL279420 IC50 = 32.36 nM 7.49
CHEMBL278957 IC50 = 34.67 nM 7.46
CHEMBL278981 IC50 = 34.67 nM 7.46
CHEMBL16494 IC50 = 60.26 nM 7.22
CHEMBL439910 IC50 = 79.43 nM 7.10
CHEMBL439908 IC50 = 89.13 nM 7.05
CHEMBL16027 IC50 = 114.82 nM 6.94
CHEMBL16330 IC50 = 114.82 nM 6.94
CHEMBL16152 IC50 = 151.36 nM 6.82
CHEMBL16456 IC50 = 173.78 nM 6.76
CHEMBL277091 IC50 = 562.34 nM 6.25
CHEMBL278049 IC50 = 1000.0 nM 6.00
CHEMBL16248 IC50 = 1000.0 nM 6.00