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Discovery and characterization of a potent and selective EP4 receptor antagonist.
Schiffler, Matthew A; Chandrasekhar, Srinivasan; Fisher, Matthew J; Harvey, Anita; Kuklish, Steven L; Wang, Xu-Shan; Warshawsky, Alan M; York, Jeremy S; Yu, Xiao-Peng.
Affiliation
  • Schiffler MA; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA. Electronic address: schifflerma@lilly.com.
  • Chandrasekhar S; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Fisher MJ; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Harvey A; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Kuklish SL; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Wang XS; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Warshawsky AM; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • York JS; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
  • Yu XP; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285 USA.
Bioorg Med Chem Lett ; 25(16): 3176-8, 2015 Aug 15.
Article in En | MEDLINE | ID: mdl-26091726
ABSTRACT
EP4 is a prostaglandin E2 receptor that is a target for potential anti-nociceptive therapy. Described herein is a class of amphoteric EP4 antagonists which reverses PGE2-induced suppression of TNFα production in human whole blood. From this class, a potent and highly bioavailable compound (6) has been selected for potential clinical studies. EP4 binding and functional data, selectivity, and pharmacokinetic properties of this compound are included.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Prostaglandin E, EP4 Subtype / Analgesics Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Prostaglandin E, EP4 Subtype / Analgesics Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article