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Assay Detail

CHEMBL5350410

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

Binding
Inhibition of ERalpha (246 to 595 residues) in doxycycline-induced human HEK293 cells incubated overnight by luciferase based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges.
Rej RK, Thomas JE, Acharyya RK, Rae JM, Wang S.
J Med Chem (2023) 66 : 8339 -8381
PubMed 37377342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.02 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1358 FULVESTRANT 4.0 1 9.30
CHEMBL4475463 AMCENESTRANT 3.0 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1358 FULVESTRANT IC50 = 0.5 nM 9.30
CHEMBL4475463 AMCENESTRANT IC50 = 1.8 nM 8.74