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Assay Detail

CHEMBL881383

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

Binding
Transcriptional activation of estrogen receptor beta in U2OS cell using estrogen-regulated luciferase reporter gene plasmid upon incubation for 20-30 mins at RT
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.
Clegg NJ, Paruthiyil S, Leitman DC, Scanlan TS.
J Med Chem (2005) 48 : 5989 -6003
PubMed 16162002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.17 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.01
CHEMBL306878 1 9.52
CHEMBL69408 1 9.52
CHEMBL371236 1 8.00
CHEMBL199140 1 7.43
CHEMBL370609 1 7.28
CHEMBL48352 1 7.27
CHEMBL371192 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.098 nM 10.01
CHEMBL306878 EC50 = 0.3 nM 9.52
CHEMBL69408 EC50 = 0.3 nM 9.52
CHEMBL371236 EC50 = 10.0 nM 8.00
CHEMBL199140 EC50 = 37.0 nM 7.43
CHEMBL370609 EC50 = 52.0 nM 7.28
CHEMBL48352 EC50 = 54.0 nM 7.27
CHEMBL371192 EC50 = 512.0 nM 6.29