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Assay Detail

CHEMBL679352

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

Functional
Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.
Lubczyk V, Bachmann H, Gust R.
J Med Chem (2002) 45 : 5358 -5364
PubMed 12431063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50995 1 8.15
CHEMBL357283 1 8.05
CHEMBL149791 1 7.82
CHEMBL150461 1 7.52
CHEMBL357824 1 7.30
CHEMBL415864 1 6.82
CHEMBL83 TAMOXIFEN 4.0 1 6.30
CHEMBL356693 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50995 IC50 = 7.0 nM 8.15
CHEMBL357283 IC50 = 9.0 nM 8.05
CHEMBL149791 IC50 = 15.0 nM 7.82
CHEMBL150461 IC50 = 30.0 nM 7.52
CHEMBL357824 IC50 = 50.0 nM 7.30
CHEMBL415864 IC50 = 150.0 nM 6.82
CHEMBL83 TAMOXIFEN IC50 = 500.0 nM 6.30
CHEMBL356693 IC50 = 500.0 nM 6.30