• Bioorg. Med. Chem. Lett. · May 2011

    Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

    • Paul R Reid, Thomas M Bridges, Douglas J Sheffler, Hyekyung P Cho, L Michelle Lewis, Emily Days, J Scott Daniels, Carrie K Jones, Colleen M Niswender, C David Weaver, P Jeffrey Conn, Craig W Lindsley, and Michael R Wood.
    • Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core, Nashville, TN 37232, USA.
    • Bioorg. Med. Chem. Lett. 2011 May 1; 21 (9): 2697-701.

    AbstractThis Letter describes a chemical lead optimization campaign directed at VU0108370, a weak M(1) PAM hit with a novel chemical scaffold from a functional HTS screen within the MLPCN. An iterative parallel synthesis approach rapidly established SAR for this series and afforded VU0405652 (ML169), a potent, selective and brain penetrant M(1) PAM with an in vitro profile comparable to the prototypical M(1) PAM, BQCA, but with an improved brain to plasma ratio.Copyright © 2010 Elsevier Ltd. All rights reserved.

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