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Assay Detail

CHEMBL676808

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Functional
Agonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Miller CP, Jirkovsky I, Tran BD, Harris HA, Moran RA, Komm BS.
Bioorg Med Chem Lett (2000) 10 : 147 -151
PubMed 10673099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.68 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627355 1 8.30
CHEMBL1627353 1 8.15
CHEMBL1628170 1 7.89
CHEMBL1628199 1 7.55
CHEMBL1627351 1 7.40
CHEMBL1627356 1 6.76
CHEMBL135 ESTRADIOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627355 EC50 = 5.0 nM 8.30
CHEMBL1627353 EC50 = 7.0 nM 8.15
CHEMBL1628170 EC50 = 13.0 nM 7.89
CHEMBL1628199 EC50 = 28.0 nM 7.55
CHEMBL1627351 EC50 = 40.0 nM 7.40
CHEMBL1627356 EC50 = 173.0 nM 6.76
CHEMBL135 ESTRADIOL EC50 = 0.007 nM -