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Assay Detail

CHEMBL679325

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

Binding
Displacement of [3H]17-beta-estradiol from human Estrogen receptor alpha
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Miller CP, Jirkovsky I, Tran BD, Harris HA, Moran RA, Komm BS.
Bioorg Med Chem Lett (2000) 10 : 147 -151
PubMed 10673099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.67 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1116 RALOXIFENE HYDROCHLORIDE 4.0 1 8.70
CHEMBL135 ESTRADIOL 4.0 1 8.52
CHEMBL1358 FULVESTRANT 4.0 1 8.22
CHEMBL1627354 1 8.05
CHEMBL1627351 1 7.50
CHEMBL1628199 1 7.48
CHEMBL33899 1 7.41
CHEMBL1628170 1 7.34
CHEMBL1627356 1 7.03
CHEMBL1627353 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1116 RALOXIFENE HYDROCHLORIDE IC50 = 2.0 nM 8.70
CHEMBL135 ESTRADIOL IC50 = 3.0 nM 8.52
CHEMBL1358 FULVESTRANT IC50 = 6.0 nM 8.22
CHEMBL1627354 IC50 = 9.0 nM 8.05
CHEMBL1627351 IC50 = 32.0 nM 7.50
CHEMBL1628199 IC50 = 33.0 nM 7.48
CHEMBL33899 IC50 = 39.0 nM 7.41
CHEMBL1628170 IC50 = 46.0 nM 7.34
CHEMBL1627356 IC50 = 94.0 nM 7.03
CHEMBL1627353 IC50 = 397.0 nM 6.40