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Assay Detail

CHEMBL678290

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Binding
Relative binding affinity for human estrogen receptor beta compared to [3H]-estradiol
6
Total Activities
6
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

Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process.
Minutolo F, Antonello M, Bertini S, Ortore G, Placanica G, Rapposelli S, Sheng S, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA, Macchia M.
J Med Chem (2003) 46 : 4032 -4042
PubMed 12954056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.75 10.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128227 1 10.32
CHEMBL335465 1 9.57
CHEMBL128654 1 8.77
CHEMBL131163 1 8.55
CHEMBL130030 1 8.28
CHEMBL135 ESTRADIOL 4.0 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128227 Ki = 0.048 nM 10.32
CHEMBL335465 Ki = 0.27 nM 9.57
CHEMBL128654 Ki = 1.7 nM 8.77
CHEMBL131163 Ki = 2.8 nM 8.55
CHEMBL130030 Ki = 5.2 nM 8.28
CHEMBL135 ESTRADIOL Ki = 100.0 nM 7.00