title: The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA. jason_imbriglio@merck.com
authors.forename: Jason E
authors.initials: JE
authors.lastname: Imbriglio
authors.forename: Daniel
authors.initials: D
authors.lastname: DiRocco
authors.forename: Rena
authors.initials: R
authors.lastname: Bodner
authors.forename: Subharekha
authors.initials: S
authors.lastname: Raghavan
authors.forename: Weichun
authors.initials: W
authors.lastname: Chen
authors.forename: Daria
authors.initials: D
authors.lastname: Marley
authors.forename: Craig
authors.initials: C
authors.lastname: Esser
authors.forename: Tom G
authors.initials: TG
authors.lastname: Holt
authors.forename: Michael S
authors.initials: MS
authors.lastname: Wolff
authors.forename: Andrew K P
authors.initials: AK
authors.lastname: Taggart
authors.forename: M Gerard
authors.initials: MG
authors.lastname: Waters
authors.forename: James R
authors.initials: JR
authors.lastname: Tata
authors.forename: Steven L
authors.initials: SL
authors.lastname: Colletti
mesh_terms: D000818:Animals; D055808:Drug Discovery; D005461:Fluorine / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D009525:Niacin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D011978:Receptors, Nicotinic
chemical_list: C530636:HCAR2 protein, human; D011725:Pyridines; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D009525:Niacin; D005461:Fluorine