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Assay Detail

CHEMBL841902

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Transcriptional potency (EC50) at Human estrogen receptor alpha
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Meyers MJ, Sun J, Carlson KE, Marriner GA, Katzenellenbogen BS, Katzenellenbogen JA.
J Med Chem (2001) 44 : 4230 -4251
PubMed 11708925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 7.91 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.74
CHEMBL135739 1 10.19
CHEMBL136039 1 9.42
CHEMBL335412 1 8.57
CHEMBL132868 1 8.54
CHEMBL334798 1 8.51
CHEMBL134938 1 8.28
CHEMBL135695 1 8.17
CHEMBL342418 2 7.85
CHEMBL135597 1 7.80
CHEMBL135649 1 7.75
CHEMBL44 GENISTEIN 2.0 1 7.70
CHEMBL334773 DIARYLPROPIONITRILE 1 7.70
CHEMBL134646 1 7.64
CHEMBL132694 1 7.40
CHEMBL335620 1 7.38
CHEMBL132919 1 7.14
CHEMBL334402 1 7.02
CHEMBL134892 1 6.89
CHEMBL137795 1 6.82
CHEMBL2111906 1 6.40
CHEMBL133203 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.018 nM 10.74
CHEMBL135739 EC50 = 0.064 nM 10.19
CHEMBL136039 EC50 = 0.38 nM 9.42
CHEMBL335412 EC50 = 2.7 nM 8.57
CHEMBL132868 EC50 = 2.9 nM 8.54
CHEMBL334798 EC50 = 3.1 nM 8.51
CHEMBL134938 EC50 = 5.2 nM 8.28
CHEMBL135695 EC50 = 6.7 nM 8.17
CHEMBL342418 EC50 = 14.0 nM 7.85
CHEMBL135597 EC50 = 16.0 nM 7.80
CHEMBL135649 EC50 = 18.0 nM 7.75
CHEMBL342418 EC50 = 18.0 nM 7.75
CHEMBL44 GENISTEIN EC50 = 20.0 nM 7.70
CHEMBL334773 DIARYLPROPIONITRILE EC50 = 20.0 nM 7.70
CHEMBL134646 EC50 = 23.0 nM 7.64
CHEMBL132694 EC50 = 40.0 nM 7.40
CHEMBL335620 EC50 = 42.0 nM 7.38
CHEMBL132919 EC50 = 73.0 nM 7.14
CHEMBL334402 EC50 = 95.0 nM 7.02
CHEMBL134892 EC50 = 130.0 nM 6.89
CHEMBL137795 EC50 = 150.0 nM 6.82
CHEMBL2111906 EC50 = 400.0 nM 6.40
CHEMBL133203 EC50 = 464.0 nM 6.33