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Assay Detail

CHEMBL1120811

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Binding
Binding affinity to ERbeta by fluorescence polarization-based competitive binding assay
8
Total Activities
8
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

Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta.
Sedlák D, Novák P, Kotora M, Bartůnek P.
J Med Chem (2010) 53 : 4290 -4294
PubMed 20408532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.93 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 7.95
CHEMBL691 ETHINYL ESTRADIOL 4.0 1 7.75
CHEMBL1098710 1 7.27
CHEMBL1097377 1 7.12
CHEMBL1094732 1 6.60
CHEMBL1098709 1 6.50
CHEMBL1097284 1 6.30
CHEMBL1096975 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 11.35 nM 7.95
CHEMBL691 ETHINYL ESTRADIOL IC50 = 17.78 nM 7.75
CHEMBL1098710 IC50 = 53.58 nM 7.27
CHEMBL1097377 IC50 = 76.38 nM 7.12
CHEMBL1094732 IC50 = 253.51 nM 6.60
CHEMBL1098709 IC50 = 319.15 nM 6.50
CHEMBL1097284 IC50 = 500.03 nM 6.30
CHEMBL1096975 IC50 = 1083.93 nM 5.96