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
2011
Lamb, Jeffrey P. | Engers, Darren W. | Niswender, Colleen M. | Rodriguez, Alice L. | Venable, Daryl F. | Conn, P Jeffrey | Lindsley, Craig W.
This Letter describes a chemical lead optimization campaign directed at a weak mGlu₅ NAM discovered while developing SAR for the mGlu₅ 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.
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