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Assay Detail

CHEMBL5337709

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

Binding
Agonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assay
2
Total Activities
2
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

Estrogen receptor (CHEMBL206)
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
EC50 2 8.73 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1405 ESTRONE 4.0 1 8.85
CHEMBL411 DIETHYLSTILBESTROL 4.0 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1405 ESTRONE EC50 = 1.4 nM 8.85
CHEMBL411 DIETHYLSTILBESTROL EC50 = 2.5 nM 8.60