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

Lookup NU author(s): Professor Mike Waring

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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.

Publication metadata

Author(s): Waring MJ, Baker DJ, Bennett SNL, Dossetter AG, Fenwick M, Garcia R, Georgsson J, Groombridge SD, Loxham S, MacFaul PA, Maskill KG, Morgan D, Morrell J, Pointon H, Robb GR, Smith DM, Stokes S, Wilkinson G

Publication type: Article

Publication status: Published

Journal: MedChemComm

Year: 2015

Issue: 6

Pages: 1024-1029

Print publication date: 01/06/2015

Online publication date: 08/04/2015

Acceptance date: 01/04/2015

ISSN (print): 2040-2503

ISSN (electronic): 2040-2511

Publisher: Royal Society of Chemistry

URL: http://dx.doi.org/10.1039/C5MD00037H

DOI: 10.1039/C5MD00037H

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