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Bioorg Med Chem Lett. 2006 Apr 1;16(7):1840-5. Epub 2006 Jan 24.

Synthesis and activity of small molecule GPR40 agonists.

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GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.


The first report on the identification and structure-activity relationships of a novel series of GPR40 agonists based on a 3-(4-{[N-alkyl]amino}phenyl)propanoic acid template is described. Structural modifications to the original screening hit yielded compounds with a 100-fold increase in potency at the human GPR40 receptor and pEC(50)s in the low nanomolar range. The carboxylic acid moiety is not critical for activity but typically elicits an agonistic response higher than those observed with carboxamide replacements. These compounds may prove useful in unraveling the therapeutic potential of this receptor for the treatment of Type 2 diabetes.

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