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Assay Detail

CHEMBL710208

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

Functional
Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF-7
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological activity of trans-2,3-dihydroraloxifene.
Schmid CR, Glasebrook AL, Misner JW, Stephenson GA.
Bioorg Med Chem Lett (1999) 9 : 1137 -1140
PubMed 10328300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.77 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537254 1 10.30
CHEMBL81 RALOXIFENE 4.0 1 9.47
CHEMBL14955 DIHYDRORALOXIFENE 1 9.28
CHEMBL83 TAMOXIFEN 4.0 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537254 IC50 = 0.05 nM 10.30
CHEMBL81 RALOXIFENE IC50 = 0.34 nM 9.47
CHEMBL14955 DIHYDRORALOXIFENE IC50 = 0.52 nM 9.28
CHEMBL83 TAMOXIFEN IC50 = 904.0 nM 6.04