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The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
Authors:Imbriglio Jason E  DiRocco Daniel  Bodner Rena  Raghavan Subharekha  Chen Weichun  Marley Daria  Esser Craig  Holt Tom G  Wolff Michael S  Taggart Andrew K P  Waters M Gerard  Tata James R  Colletti Steven L
Affiliation:a Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA
b Department of Drug Metabolism, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA
c Department of Cardiovascular Diseases, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA
Abstract:Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.
Keywords:Niacin   Atherosclerosis   Anthranilic acid
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