| Literature DB >> 22884988 |
Mike Lizarzaburu1, Simon Turcotte, Xiaohui Du, Jason Duquette, Angela Fu, Jonathan Houze, Leping Li, Jinqian Liu, Michiko Murakoshi, Kozo Oda, Ryo Okuyama, Futoshi Nara, Jeff Reagan, Ming Yu, Julio C Medina.
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.Entities:
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Year: 2012 PMID： 22884988 DOI： 10.1016/j.bmcl.2012.07.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823