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Assay Detail

CHEMBL868725

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

Functional
Effect on ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter
4
Total Activities
4
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

Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P.
Bioorg Med Chem Lett (2005) 15 : 5562 -5566
PubMed 16219463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.34 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 11.00
CHEMBL371012 1 7.42
CHEMBL200799 1 6.61
CHEMBL199599 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.01 nM 11.00
CHEMBL371012 EC50 = 38.5 nM 7.42
CHEMBL200799 EC50 = 243.0 nM 6.61
CHEMBL199599 EC50 > 1000.0 nM -