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Assay Detail

CHEMBL872717

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Functional
Apparent binding affinity against estradiol-stimulated T-47D cell proliferation
5
Total Activities
5
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
Ki 5 9.97 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68055 ACOLBIFENE 3.0 1 10.82
CHEMBL308234 1 10.80
CHEMBL291808 1 10.55
CHEMBL67783 1 9.28
CHEMBL441622 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68055 ACOLBIFENE Ki = 0.015 nM 10.82
CHEMBL308234 Ki = 0.016 nM 10.80
CHEMBL291808 Ki = 0.028 nM 10.55
CHEMBL67783 Ki = 0.525 nM 9.28
CHEMBL441622 Ki = 4.22 nM 8.38