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Assay Detail

CHEMBL5334565

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

Binding
Irreversible inhibition of human STS expressed in human T47D cells using [3H]E1S as substrate preincubated for 2 hr followed by substrate addition measured after 24 hrs in presence of E1S by HPLC analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for <i>In Vivo</i> Proof-of-Principle Studies in an Endometriosis Mouse Model.
Salah M, Tahoun M, Rudzitis-Auth J, Stotz L, van Koppen CJ, Laschke MW, Abdelsamie AS, Frotscher M.
J Med Chem (2023) 66 : 8975 -8992
PubMed 37369108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.91 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071245 1 7.80
CHEMBL5394384 1 7.10
CHEMBL5429832 1 6.38
CHEMBL5440157 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071245 IC50 = 16.0 nM 7.80
CHEMBL5394384 IC50 = 79.0 nM 7.10
CHEMBL5429832 IC50 = 420.0 nM 6.38
CHEMBL5440157 IC50 = 460.0 nM 6.34