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Assay Detail

CHEMBL2051159

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

Binding
Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs.
Chalmers MJ, Wang Y, Novick S, Sato M, Bryant HU, Montrose-Rafizdeh C, Griffin PR, Dodge JA.
ACS Med Chem Lett (2012) 3 : 207 -210
PubMed 22582136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.44 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83 TAMOXIFEN 4.0 1 9.29
CHEMBL81 RALOXIFENE 4.0 1 8.56
CHEMBL46937 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83 TAMOXIFEN Ki = 0.51 nM 9.29
CHEMBL81 RALOXIFENE Ki = 2.74 nM 8.56
CHEMBL46937 Ki = 35.0 nM 7.46