Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

Thomas M. Bridges, J. Phillip Kennedy, Corey R. Hopkins, P. Jeffrey Conn, Craig W. Lindsley

Research output: Contribution to journalArticle

22 Scopus citations


This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M5-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan Gq mAChR M1, M3, M5 PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties.

Original languageEnglish (US)
Pages (from-to)5617-5622
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number19
StatePublished - Oct 1 2010


  • Allosteric
  • M5
  • PAM
  • mAChR

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Heterobiaryl and heterobiaryl ether derived M<sub>5</sub> positive allosteric modulators'. Together they form a unique fingerprint.

  • Cite this