1310486-20-4Relevant articles and documents
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists
Lamb, Jeffrey P.,Engers, Darren W.,Niswender, Colleen M.,Rodriguez, Alice L.,Venable, Daryl F.,Conn, Jeffrey P.,Lindsley, Craig W.
, p. 2711 - 2714 (2011/06/20)
This Letter describes a chemical lead optimization campaign directed at a weak mGlu5 NAM discovered while developing SAR for the mGlu 5 PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu5 NAMs, mGlu5 PAMs as well as mGlu5 partial antagonists.