Home
Resources
Publications
Discovery and Optimization of a Novel, Selective and Brain Penetrant M1 Positive Allosteric Modulator (PAM): The Development of ML169, an MLPCN Probe

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, Michael R Wood

Bioorg Med Chem Lett. 2011 May 1;21(9):2697-701.

PMID: 21194936

Abstract:

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 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1222878025	ML169		1222878-02-5	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: