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Assay Detail

CHEMBL4051802

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

Binding
Inhibition of human placental microsomal STS assessed as formation of E1 preincubated for 30 mins followed by addition of E1S as substrate measured after 20 mins by ELISA
10
Total Activities
10
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 10 7.18 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286738 IROSUSTAT 2.0 1 7.82
CHEMBL4091943 1 7.71
CHEMBL4064200 1 7.71
CHEMBL4084183 1 7.46
CHEMBL4102153 1 7.09
CHEMBL4099681 1 6.98
CHEMBL4066635 1 6.91
CHEMBL4071245 1 6.84
CHEMBL4083248 1 6.66
CHEMBL4072794 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286738 IROSUSTAT IC50 = 15.1 nM 7.82
CHEMBL4091943 IC50 = 19.5 nM 7.71
CHEMBL4064200 IC50 = 19.4 nM 7.71
CHEMBL4084183 IC50 = 35.0 nM 7.46
CHEMBL4102153 IC50 = 81.8 nM 7.09
CHEMBL4099681 IC50 = 105.5 nM 6.98
CHEMBL4066635 IC50 = 123.4 nM 6.91
CHEMBL4071245 IC50 = 143.1 nM 6.84
CHEMBL4083248 IC50 = 220.8 nM 6.66
CHEMBL4072794 IC50 = 244.5 nM 6.61