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Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
Blanco, Maria-Jesus; Vetman, Tatiana; Chandrasekhar, Srinivasan; Fisher, Matthew J; Harvey, Anita; Mudra, Daniel; Wang, Xu-Shan; Yu, Xiao-Peng; Schiffler, Matthew A; Warshawsky, Alan M.
Affiliation
  • Blanco MJ; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States. Electronic address: blanco_maria@lilly.com.
  • Vetman T; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Chandrasekhar S; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Fisher MJ; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Harvey A; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Mudra D; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Wang XS; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Yu XP; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Schiffler MA; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Warshawsky AM; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
Bioorg Med Chem Lett ; 26(1): 105-9, 2016 Jan 01.
Article in En | MEDLINE | ID: mdl-26608552
ABSTRACT
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profiles of this compound are discussed.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzoates / Drug Discovery / Receptors, Prostaglandin E, EP4 Subtype / Naphthalenes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Publication country: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzoates / Drug Discovery / Receptors, Prostaglandin E, EP4 Subtype / Naphthalenes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Publication country: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM