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Assay Detail

CHEMBL678093

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Binding
Binding affinity towards human estrogen receptor beta (ERbeta)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
Chen HY, Kim S, Wu JY, Birzin ET, Chan W, Yang YT, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2004) 14 : 2551 -2554
PubMed 15109649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.96 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 7.92
CHEMBL85090 1 7.80
CHEMBL316132 1 7.55
CHEMBL431611 1 7.51
CHEMBL315271 1 7.47
CHEMBL85650 1 7.42
CHEMBL85881 1 7.40
CHEMBL419110 1 7.37
CHEMBL85536 1 7.22
CHEMBL313825 1 6.98
CHEMBL304552 1 6.84
CHEMBL83623 1 6.79
CHEMBL313941 1 6.51
CHEMBL315761 1 6.44
CHEMBL83451 1 5.09
CHEMBL83060 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE IC50 = 12.0 nM 7.92
CHEMBL85090 IC50 = 16.0 nM 7.80
CHEMBL316132 IC50 = 28.0 nM 7.55
CHEMBL431611 IC50 = 31.0 nM 7.51
CHEMBL315271 IC50 = 34.0 nM 7.47
CHEMBL85650 IC50 = 38.0 nM 7.42
CHEMBL85881 IC50 = 40.0 nM 7.40
CHEMBL419110 IC50 = 43.0 nM 7.37
CHEMBL85536 IC50 = 60.0 nM 7.22
CHEMBL313825 IC50 = 105.0 nM 6.98
CHEMBL304552 IC50 = 143.0 nM 6.84
CHEMBL83623 IC50 = 162.0 nM 6.79
CHEMBL313941 IC50 = 308.0 nM 6.51
CHEMBL315761 IC50 = 361.0 nM 6.44
CHEMBL83451 IC50 = 8202.0 nM 5.09
CHEMBL83060 IC50 = 8254.0 nM 5.08