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Assay Detail

CHEMBL4716150

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

Binding
Displacement of ES2 from recombinant human ER-beta incubated for 2 hrs by fluorescence based assay
6
Total Activities
6
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 beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.
Lv W,Liu J,Skaar TC,O'Neill E,Yu G,Flockhart DA,Cushman M
J Med Chem (2016) 59 : 157 -170
PubMed 26704594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.80 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4777271 1 7.39
CHEMBL4753594 1 7.25
CHEMBL4780337 1 7.13
CHEMBL4755831 1 6.53
CHEMBL149791 1 6.51
CHEMBL4749692 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4777271 EC50 = 40.9 nM 7.39
CHEMBL4753594 EC50 = 56.3 nM 7.25
CHEMBL4780337 EC50 = 73.6 nM 7.13
CHEMBL4755831 EC50 = 296.0 nM 6.53
CHEMBL149791 EC50 = 307.0 nM 6.51
CHEMBL4749692 EC50 = 1080.0 nM 5.97