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Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
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Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs)

Anthony L Handlon1, Lee T Schaller1, Lisa M Leesnitzer1

  • 1Metabolic Pathways Cardiovascular Unit and Platform Technology & Science, GlaxoSmithKline , 709 Swedeland Road, King of Prussia, Pennsylvania 19406-0939, United States.

ACS Medicinal Chemistry Letters
|January 29, 2016
PubMed
Summary

Researchers developed potent selective androgen receptor modulators (SARMs) using a novel core structure. Optimization guided by lipophilic ligand efficiency (LLE) yielded a SARM with nanomolar potency and excellent drug-like properties.

Keywords:
LLESARMandrogen receptorligand efficiencyselective androgen receptor modulator

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