2. Academic Validation
  3. Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists

Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):105-9. doi: 10.1016/j.bmcl.2015.11.023.
Maria-Jesus Blanco 1,  Tatiana Vetman 2,  Srinivasan Chandrasekhar 2,  Matthew J Fisher 2,  Anita Harvey 2,  Daniel Mudra 2,  Xu-Shan Wang 2,  Xiao-Peng Yu 2,  Matthew A Schiffler 2,  Alan M Warshawsky 2
Affiliations

Affiliations

  • 1 Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States. Electronic address: [email protected].
  • 2 Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
PMID: 26608552 DOI: 10.1016/j.bmcl.2015.11.023
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.

Keywords

Arthritis pain; EP4 receptor antagonist; Human whole blood assay; Prostaglandin E2.

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