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Assay Detail

CHEMBL891639

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Binding
Inhibition of human ERbeta by radioligand binding assay
12
Total Activities
12
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

ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.
Mewshaw RE, Bowen SM, Harris HA, Xu ZB, Manas ES, Cohn ST.
Bioorg Med Chem Lett (2007) 17 : 902 -906
PubMed 17188490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.92 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.44
CHEMBL231811 1 8.40
CHEMBL394357 1 8.40
CHEMBL231810 1 8.40
CHEMBL395308 1 8.30
CHEMBL232023 1 8.09
CHEMBL438516 1 8.05
CHEMBL44 GENISTEIN 2.0 1 8.01
CHEMBL231812 1 8.00
CHEMBL388418 1 7.92
CHEMBL232022 1 6.70
CHEMBL394614 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 3.6 nM 8.44
CHEMBL231811 IC50 = 4.0 nM 8.40
CHEMBL394357 IC50 = 4.0 nM 8.40
CHEMBL231810 IC50 = 4.0 nM 8.40
CHEMBL395308 IC50 = 5.0 nM 8.30
CHEMBL232023 IC50 = 8.05 nM 8.09
CHEMBL438516 IC50 = 9.0 nM 8.05
CHEMBL44 GENISTEIN IC50 = 9.7 nM 8.01
CHEMBL231812 IC50 = 10.0 nM 8.00
CHEMBL388418 IC50 = 12.0 nM 7.92
CHEMBL232022 IC50 = 202.0 nM 6.70
CHEMBL394614 IC50 = 457.0 nM 6.34