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Assay Detail

CHEMBL4051809

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

Binding
Inhibition of 17beta-HSD1 in human T47D cells preincubated for 1 hr followed by addition of [3H]-E1/E1 as substrate measured after 30 mins by HPLC based radio-detection method
5
Total Activities
5
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 1 (CHEMBL3181)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
Salah M, Abdelsamie AS, Frotscher M.
J Med Chem (2017) 60 : 4086 -4092
PubMed 28406629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.61 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071588 1 8.10
CHEMBL4102153 1 7.70
CHEMBL4071245 1 7.65
CHEMBL4091943 1 7.38
CHEMBL4064200 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071588 IC50 = 7.9 nM 8.10
CHEMBL4102153 IC50 = 20.0 nM 7.70
CHEMBL4071245 IC50 = 22.2 nM 7.65
CHEMBL4091943 IC50 = 42.1 nM 7.38
CHEMBL4064200 IC50 = 60.9 nM 7.21