Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4051807

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

Binding
Inhibition of STS in human T47D cells preincubated for 1 hr followed by addition of [3H]-E1S/E1S as substrate measured after 24 hrs 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

Steryl-sulfatase (CHEMBL3559)
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 8.39 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286738 IROSUSTAT 2.0 1 8.72
CHEMBL4091943 1 8.68
CHEMBL4064200 1 8.47
CHEMBL4102153 1 8.29
CHEMBL4071245 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286738 IROSUSTAT IC50 = 1.9 nM 8.72
CHEMBL4091943 IC50 = 2.1 nM 8.68
CHEMBL4064200 IC50 = 3.4 nM 8.47
CHEMBL4102153 IC50 = 5.1 nM 8.29
CHEMBL4071245 IC50 = 15.6 nM 7.81