1224952-64-0Relevant articles and documents
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: Development of a potent and highly selective M1 PAM
Bridges, Thomas M.,Phillip Kennedy,Noetzel, Meredith J.,Breininger, Micah L.,Gentry, Patrick R.,Jeffrey Conn,Lindsley, Craig W.
scheme or table, p. 1972 - 1975 (2010/09/15)
This Letter describes a chemical lead optimization campaign directed at VU0119498, a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) with the goal of developing a selective M1 PAM. An iterative library synthesis approach delivered a potent (M1 EC50 = 830 nM) and highly selective M1 PAM (>30 μM vs M2-M5).