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Assay Detail

CHEMBL682170

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Binding
Binding affinity for human estrogen receptor beta
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.
Tan Q, Birzin ET, Chan W, Tien Yang Y, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2004) 14 : 3747 -3751
PubMed 15203155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.06 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.96
CHEMBL122208 1 7.57
CHEMBL121720 1 7.57
CHEMBL334096 1 7.51
CHEMBL304552 1 7.35
CHEMBL121978 1 7.23
CHEMBL125119 1 6.94
CHEMBL340606 1 6.79
CHEMBL124474 1 6.73
CHEMBL332625 1 6.73
CHEMBL122237 1 6.59
CHEMBL121879 1 6.44
CHEMBL340111 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 1.1 nM 8.96
CHEMBL122208 IC50 = 27.0 nM 7.57
CHEMBL121720 IC50 = 27.0 nM 7.57
CHEMBL334096 IC50 = 31.0 nM 7.51
CHEMBL304552 IC50 = 45.0 nM 7.35
CHEMBL121978 IC50 = 59.0 nM 7.23
CHEMBL125119 IC50 = 115.0 nM 6.94
CHEMBL340606 IC50 = 161.0 nM 6.79
CHEMBL124474 IC50 = 186.0 nM 6.73
CHEMBL332625 IC50 = 186.0 nM 6.73
CHEMBL122237 IC50 = 259.0 nM 6.59
CHEMBL121879 IC50 = 365.0 nM 6.44
CHEMBL340111 IC50 = 4372.0 nM 5.36