2. Academic Validation
  3. Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain

Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. doi: 10.1016/j.bmcl.2010.04.065.
John Colucci 1,  Michael Boyd,  Carl Berthelette,  Jean-Francois Chiasson,  Zhaoyin Wang,  Yves Ducharme,  Rick Friesen,  Mark Wrona,  Jean-Francois Levesque,  Danielle Denis,  Marie-Claude Mathieu,  Rino Stocco,  Alex G Therien,  Patsy Clarke,  Steve Rowland,  Daigen Xu,  Yongxin Han
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Frosst Canada Ltd, Kirkland, Quebec, Canada.
PMID: 20471829 DOI: 10.1016/j.bmcl.2010.04.065
Abstract

The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model.

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