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Assay Detail

CHEMBL904965

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

Binding
Displacement of [3H]estradiol from human recombinant ERbeta
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
Qin Z, Kastrati I, Chandrasena RE, Liu H, Yao P, Petukhov PA, Bolton JL, Thatcher GR.
J Med Chem (2007) 50 : 2682 -2692
PubMed 17489582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.96 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226268 1 8.02
CHEMBL226327 1 7.79
CHEMBL226269 1 7.55
CHEMBL226329 1 7.31
CHEMBL389683 1 7.18
CHEMBL226267 ARZOXIFENE 3.0 1 7.18
CHEMBL81 RALOXIFENE 4.0 1 6.25
CHEMBL389907 1 5.75
CHEMBL449038 1 5.63
CHEMBL226379 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226268 IC50 = 9.6 nM 8.02
CHEMBL226327 IC50 = 16.3 nM 7.79
CHEMBL226269 IC50 = 27.9 nM 7.55
CHEMBL226329 IC50 = 48.6 nM 7.31
CHEMBL389683 IC50 = 66.7 nM 7.18
CHEMBL226267 ARZOXIFENE IC50 = 66.3 nM 7.18
CHEMBL81 RALOXIFENE IC50 = 557.0 nM 6.25
CHEMBL389907 IC50 = 1800.0 nM 5.75
CHEMBL449038 IC50 = 2360.0 nM 5.63
CHEMBL226379 IC50 > 1600.0 nM -