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Assay Detail

CHEMBL683103

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

Binding
Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 2.5%DMF
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Uterus
Subcellular Cytosol
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 3 9.55 10.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68055 ACOLBIFENE 3.0 1 10.16
CHEMBL135 ESTRADIOL 4.0 1 9.74
CHEMBL1222035 1 8.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68055 ACOLBIFENE Ki = 0.069 nM 10.16
CHEMBL135 ESTRADIOL Ki = 0.181 nM 9.74
CHEMBL1222035 Ki = 1.76 nM 8.75