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Assay Detail

CHEMBL3242833

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

Binding
Antagonist activity at human Gal4-fused ER-alpha expressed in HEK293 cells assessed as inhibition of 17beta-estradiol-induced effect by luciferase reporter gene assay
7
Total Activities
7
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

Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
Kajita D, Nakamura M, Matsumoto Y, Makishima M, Hashimoto Y.
Bioorg Med Chem (2014) 22 : 2244 -2252
PubMed 24630694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.66 8.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2403355 1 8.45
CHEMBL2403356 1 8.31
CHEMBL2403357 1 7.85
CHEMBL3235686 1 7.58
CHEMBL2403349 1 7.53
CHEMBL3235685 1 6.94
CHEMBL1782331 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2403355 IC50 = 3.53 nM 8.45
CHEMBL2403356 IC50 = 4.92 nM 8.31
CHEMBL2403357 IC50 = 14.0 nM 7.85
CHEMBL3235686 IC50 = 26.2 nM 7.58
CHEMBL2403349 IC50 = 29.7 nM 7.53
CHEMBL3235685 IC50 = 115.0 nM 6.94
CHEMBL1782331 IC50 = 118.0 nM 6.93