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Assay Detail

CHEMBL2387873

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

Binding
Displacement of fluorescent ES2 from human recombinant ERalpha after 2 hrs by fluorimetric analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Lv W, Liu J, Lu D, Flockhart DA, Cushman M.
J Med Chem (2013) 56 : 4611 -4618
PubMed 23731360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.52 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386284 1 7.77
CHEMBL3350384 1 7.57
CHEMBL2386285 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386284 EC50 = 17.0 nM 7.77
CHEMBL3350384 EC50 = 26.9 nM 7.57
CHEMBL2386285 EC50 = 58.7 nM 7.23