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Assay Detail

CHEMBL829092

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

Binding
Inhibition of [3H]17-beta-estradiol binding to mouse ER beta expressed in Escherichia coli
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor beta (CHEMBL2995)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Malamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC, Harris HA.
J Med Chem (2004) 47 : 5021 -5040
PubMed 15456246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.27 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188528 1 8.77
CHEMBL135 ESTRADIOL 4.0 1 8.64
CHEMBL187207 1 8.57
CHEMBL450940 PRINABEREL 2.0 1 8.43
CHEMBL186513 1 8.37
CHEMBL187673 1 8.02
CHEMBL187392 1 8.00
CHEMBL188882 1 7.89
CHEMBL188230 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188528 IC50 = 1.7 nM 8.77
CHEMBL135 ESTRADIOL IC50 = 2.3 nM 8.64
CHEMBL187207 IC50 = 2.7 nM 8.57
CHEMBL450940 PRINABEREL IC50 = 3.7 nM 8.43
CHEMBL186513 IC50 = 4.3 nM 8.37
CHEMBL187673 IC50 = 9.5 nM 8.02
CHEMBL187392 IC50 = 9.9 nM 8.00
CHEMBL188882 IC50 = 13.0 nM 7.89
CHEMBL188230 IC50 = 16.5 nM 7.78