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Assay Detail

CHEMBL810263

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

Binding
Compound was tested for its ability to inhibit human embryonal kidney cell derived steroid sulfatase activity in transforming [3H]E1S (estrone sulfate) to E1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type kidney
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Steryl-sulfatase (CHEMBL3559)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol.
Ciobanu LC, Boivin RP, Luu-The V, Labrie F, Poirier D.
J Med Chem (1999) 42 : 2280 -2286
PubMed 10377235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.53 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627465 1 9.82
CHEMBL1627878 1 9.41
CHEMBL122708 EMATE 1 8.68
CHEMBL518966 1 8.08
CHEMBL482212 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627465 IC50 = 0.15 nM 9.82
CHEMBL1627878 IC50 = 0.39 nM 9.41
CHEMBL122708 EMATE IC50 = 2.1 nM 8.68
CHEMBL518966 IC50 = 8.3 nM 8.08
CHEMBL482212 IC50 = 230.0 nM 6.64