Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40

A series of 2-(pyridinyl)pyrimidines were identified as potent GPR40 antagonists. Despite significant challenges related to improving the combination of potency and lipophilicity within the series, the compounds were optimised to identify a suitable in vivo probe compound, which was confirmed to exh...

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Bibliographic Details
Published in:MedChemComm 2015-01, Vol.6 (6), p.1024-1029
Main Authors: Waring, Michael J., Baker, David J., Bennett, Stuart N. L., Dossetter, Alexander G., Fenwick, Mark, Garcia, Rob, Georgsson, Jennie, Groombridge, Sam D., Loxham, Susan, MacFaul, Philip A., Maskill, Katie G., Morgan, David, Morrell, Jenny, Pointon, Helen, Robb, Graeme R., Smith, David M., Stokes, Stephen, Wilkinson, Gary
Format: Article
Language:English
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Summary:A series of 2-(pyridinyl)pyrimidines were identified as potent GPR40 antagonists. Despite significant challenges related to improving the combination of potency and lipophilicity within the series, the compounds were optimised to identify a suitable in vivo probe compound, which was confirmed to exhibit pharmacology consistent with GPR40 antagonism.
ISSN:2040-2503
2040-2511
DOI:10.1039/C5MD00037H