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Assay Detail

CHEMBL828612

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

Binding
Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 37 degree C pH7.4
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

17-beta-hydroxysteroid dehydrogenase type 3 (CHEMBL4234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship.
Tchédam Ngatcha B, Luu-The V, Labrie F, Poirier D.
J Med Chem (2005) 48 : 5257 -5268
PubMed 16078844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.89 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137852 1 7.24
CHEMBL3138113 1 7.22
CHEMBL3137851 1 7.17
CHEMBL3138219 1 7.14
CHEMBL3138082 1 7.14
CHEMBL3138431 1 7.09
CHEMBL3137857 1 7.06
CHEMBL3138210 1 7.01
CHEMBL3137845 1 7.00
CHEMBL3137856 1 7.00
CHEMBL3138330 1 6.94
CHEMBL3138065 1 6.85
CHEMBL3138209 1 6.83
CHEMBL3138398 1 6.81
CHEMBL85799 ETIOCHOLANOLONE 1 6.48
CHEMBL3138336 1 6.45
CHEMBL3138074 1 6.45
CHEMBL274826 ANDROSTENEDIONE -1.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137852 IC50 = 57.0 nM 7.24
CHEMBL3138113 IC50 = 60.0 nM 7.22
CHEMBL3137851 IC50 = 67.0 nM 7.17
CHEMBL3138219 IC50 = 73.0 nM 7.14
CHEMBL3138082 IC50 = 73.0 nM 7.14
CHEMBL3138431 IC50 = 81.0 nM 7.09
CHEMBL3137857 IC50 = 87.0 nM 7.06
CHEMBL3138210 IC50 = 97.0 nM 7.01
CHEMBL3137845 IC50 = 99.0 nM 7.00
CHEMBL3137856 IC50 = 100.0 nM 7.00
CHEMBL3138330 IC50 = 116.0 nM 6.94
CHEMBL3138065 IC50 = 142.0 nM 6.85
CHEMBL3138209 IC50 = 147.0 nM 6.83
CHEMBL3138398 IC50 = 154.0 nM 6.81
CHEMBL85799 ETIOCHOLANOLONE IC50 = 330.0 nM 6.48
CHEMBL3138336 IC50 = 352.0 nM 6.45
CHEMBL3138074 IC50 = 354.0 nM 6.45
CHEMBL274826 ANDROSTENEDIONE IC50 = 758.0 nM 6.12