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Assay Detail

CHEMBL813050

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Functional
Inhibition of estradiol-stimulated T-47D cell proliferation.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T-47D
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.
Gauthier S, Caron B, Cloutier J, Dory YL, Favre A, Larouche D, Mailhot J, Ouellet C, Schwerdtfeger A, Leblanc G, Martel C, Simard J, Mérand Y, Bélanger A, Labrie C, Labrie F.
J Med Chem (1997) 40 : 2117 -2122
PubMed 9216828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.86 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308234 1 9.85
CHEMBL68055 ACOLBIFENE 3.0 1 9.85
CHEMBL291808 1 9.61
CHEMBL67783 1 8.34
CHEMBL67837 1 8.08
CHEMBL441622 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308234 IC50 = 0.14 nM 9.85
CHEMBL68055 ACOLBIFENE IC50 = 0.14 nM 9.85
CHEMBL291808 IC50 = 0.243 nM 9.61
CHEMBL67783 IC50 = 4.6 nM 8.34
CHEMBL67837 IC50 = 8.4 nM 8.08
CHEMBL441622 IC50 = 36.2 nM 7.44