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Assay Detail

CHEMBL5337701

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

Binding
Inhibition of STS in human JEG-3 cells assessed as inhibition of estrone E1 formation using [3H]estrone sulfate as substrate incubated for 20 hrs in presence of E1S by scintillation spectrometry
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type JEG-3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Zaraei SO, Dohle W, Anbar HS, El-Gamal R, Leblond B, Foster PA, Al-Tel TH, Potter BVL, El-Gamal MI.
Bioorg Med Chem (2024) 101 : 117645 -117645
PubMed 38401456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.32 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286738 IROSUSTAT 2.0 1 8.68
CHEMBL5436409 1 7.91
CHEMBL5413467 1 6.48
CHEMBL5408262 1 6.22
CHEMBL81 RALOXIFENE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286738 IROSUSTAT IC50 = 2.1 nM 8.68
CHEMBL5436409 IC50 = 12.2 nM 7.91
CHEMBL5413467 IC50 = 332.0 nM 6.48
CHEMBL5408262 IC50 = 607.0 nM 6.22
CHEMBL81 RALOXIFENE IC50 - -