VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively[1][2].
VU0238441 is a positive allosteric modulator (PAM) of pan-muscarinic acetylcholine receptor (mAChR) with EC50 values of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and > 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and > for M5, M3, M2, M1 and M4, respectively 10 μM.
[1] Thomas M Bridges, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. DOI:
10.1016/j.bmcl.2009.11.089[2] Thomas M Bridges, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. DOI:
10.1021/jm900286j
