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Assay Detail

CHEMBL1919075

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

Binding
Inhibition of human placental microsomal 17beta-HSD2 using [3H]E2 as substrate by HPLC analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

17-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL2789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors.
Wetzel M, Marchais-Oberwinkler S, Perspicace E, Möller G, Adamski J, Hartmann RW.
J Med Chem (2011) 54 : 7547 -7557
PubMed 21972996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.75 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1917897 1 7.72
CHEMBL1917889 1 6.88
CHEMBL1917895 1 6.81
CHEMBL1917893 1 6.62
CHEMBL1917887 1 6.58
CHEMBL1917881 1 6.56
CHEMBL1917891 1 6.54
CHEMBL193726 1 6.52
CHEMBL1917898 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1917897 IC50 = 19.0 nM 7.72
CHEMBL1917889 IC50 = 132.0 nM 6.88
CHEMBL1917895 IC50 = 156.0 nM 6.81
CHEMBL1917893 IC50 = 238.0 nM 6.62
CHEMBL1917887 IC50 = 261.0 nM 6.58
CHEMBL1917881 IC50 = 275.0 nM 6.56
CHEMBL1917891 IC50 = 292.0 nM 6.54
CHEMBL193726 IC50 = 302.0 nM 6.52
CHEMBL1917898 IC50 = 307.0 nM 6.51