The discovery and synthesis of a series of (dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists from a small-molecule combinatorial library using a high-throughput calcium mobilization functional assay (HEK293-human OX2-R cell line) is described. Active compounds show a good correlation between high-throughput single concentration screening data and measured IC(50)s. Specific examples exhibit IC(50) values of approximately 20 nM using human orexin A as the peptide agonist for the orexin-2 receptor.
Maria L. Webb合作论文数2zhao jiuquao合作论文数1Ian Henderson合作论文数1John E. Tellew合作论文数1John J. Baldwin合作论文数1Srilatha Simhadri合作论文数1Lan-Ying Qin合作论文数1Ilana L. Stroke合作论文数1Frank S. Waksmunski合作论文数1Marc-Raleigh Brescia合作论文数1John Saunders合作论文数1Kenneth C. Appell合作论文数1Robert Horlick合作论文数1
John P Williams合作论文数1Andrew G. Cole合作论文数1
