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Assay Detail

CHEMBL1925012

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Binding
Inhibition of ERalpha
10
Total Activities
10
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 (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of the diastereomerism of dihydrobenzoxathiin SERMs for ER alpha by molecular modeling.
Zhuang S, Zhang J, Zhang F, Zhang Z, Wen Y, Liu W.
Bioorg Med Chem Lett (2011) 21 : 7298 -7305
PubMed 22061644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 9.09 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183467 1 9.40
CHEMBL182980 1 9.30
CHEMBL367350 1 9.30
CHEMBL182794 1 9.30
CHEMBL367574 1 9.15
CHEMBL369545 1 9.15
CHEMBL183263 1 9.15
CHEMBL180300 1 8.89
CHEMBL180792 1 8.77
CHEMBL183584 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183467 IC50 = 0.4 nM 9.40
CHEMBL182980 IC50 = 0.5 nM 9.30
CHEMBL367350 IC50 = 0.5 nM 9.30
CHEMBL182794 IC50 = 0.5 nM 9.30
CHEMBL367574 IC50 = 0.7 nM 9.15
CHEMBL369545 IC50 = 0.7 nM 9.15
CHEMBL183263 IC50 = 0.7 nM 9.15
CHEMBL180300 IC50 = 1.3 nM 8.89
CHEMBL180792 IC50 = 1.7 nM 8.77
CHEMBL183584 IC50 = 3.0 nM 8.52