Discovery and optimization of a novel, selective and brain penetrant M(1) positive allosteric modulator (PAM): the development of ML169, an MLPCN Probe

This 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 pote...

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Main Authors: Reid, Paul R., Bridges, Thomas M., Sheffler, Douglas J., Cho, Hyekyung P., Lewis, L. Michelle, Days, Emily, Daniels, J. Scott, Jones, Carrie K., Niswender, Colleen M., Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2010
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3082000/
https://ncbi.nlm.nih.gov/pubmed/21194936
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2010.12.015
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