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Issue 6, 2015
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Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40

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Abstract

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.

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

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Supplementary files

Article information


Submitted
28 Jan 2015
Accepted
01 Apr 2015
First published
08 Apr 2015

Med. Chem. Commun., 2015,6, 1024-1029
Article type
Concise Article
Author version available

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

M. J. Waring, D. J. Baker, S. N. L. Bennett, A. G. Dossetter, M. Fenwick, R. Garcia, J. Georgsson, S. D. Groombridge, S. Loxham, P. A. MacFaul, K. G. Maskill, D. Morgan, J. Morrell, H. Pointon, G. R. Robb, D. M. Smith, S. Stokes and G. Wilkinson, Med. Chem. Commun., 2015, 6, 1024
DOI: 10.1039/C5MD00037H

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