A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies

Craig Jamieson, Stephanie Basten, Robert A. Campbell, Iain A. Cumming, Kevin J. Gillen, Jonathan Gillespie, Bert Kazemier, Michael Kiczun, Yvonne Lamont, Amanda J. Lyons, John K.F. Maclean, Elizabeth M. Moir, John A. Morrow, Marianthi Papakosta, Zoran Rankovic, Lynn Smith

Research output: Contribution to journalArticle

31 Citations (Scopus)
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Abstract

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.
Original languageEnglish
Pages (from-to)5753-5756
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
Early online date13 Aug 2010
DOIs
Publication statusPublished - 1 Oct 2010

Keywords

  • AMPA receptor
  • hit-to-lead
  • SBDD
  • allosteric modulator

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