Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand

被引:26
作者
Wolkenberg, Scott E.
Zhao, Zhijian
Kapitskaya, Arianna
Webber, Andrea L.
Petrukhin, Konstantin
Tang, Yui Sing
Dean, Dennis C.
Hartman, George D.
Lindsley, Craig W.
机构
[1] Merck & Co Inc, Dept Med Chem, Technol Enabled Synth Grp, West Point, PA 19486 USA
[2] Merck & Co Inc, Dept Ophthalm Res, West Point, PA 19486 USA
[3] Merck & Co Inc, Dept Drug Metab, Rahway, NJ 07065 USA
关键词
NR2E3; PNR; RNR; age-related macular degeneration; AMD; nuclear receptor; ophthalmics;
D O I
10.1016/j.bmcl.2006.07.056
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Agonists of NR2E3 (PNR, RNR) have been identified and optimized to EC50 < 200 nM. A tritiated analogue of one agonist was prepared to aid in the development of a binding assay. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5001 / 5004
页数:4
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