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Bioorg Med Chem Lett. 2012 Sep 15;22(18):5942-7. doi: 10.1016/j.bmcl.2012.07.063. Epub 2012 Jul 23.

Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.

Author information

1
Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA. mlizarza@amgen.com

Abstract

The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described.

PMID:
22884988
DOI:
10.1016/j.bmcl.2012.07.063
[Indexed for MEDLINE]
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