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Assay Detail

CHEMBL3429913

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

Binding
Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Degorce SL, Bailey A, Callis R, De Savi C, Ducray R, Lamont G, MacFaul P, Maudet M, Martin S, Morgentin R, Norman RA, Peru A, Pink JH, Plé PA, Roberts B, Scott JS.
J Med Chem (2015) 58 : 3522 -3533
PubMed 25790336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.99 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3427402 1 8.41
CHEMBL3427401 1 7.57
CHEMBL33899 1 -
CHEMBL195515 1 -
CHEMBL3427385 1 -
CHEMBL3427414 1 -
CHEMBL3427415 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3427402 IC50 = 3.9 nM 8.41
CHEMBL3427401 IC50 = 27.0 nM 7.57
CHEMBL33899 IC50 > 100000.0 nM -
CHEMBL195515 IC50 > 30000.0 nM -
CHEMBL3427385 IC50 > 100000.0 nM -
CHEMBL3427414 IC50 > 3100.0 nM -
CHEMBL3427415 IC50 > 3100.0 nM -