title: Tetrahydroquinoline derivatives as CRTH2 antagonists.
abstract: A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.
authors.affiliation: Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jiwenl@amgen.com
authors.forename: Jiwen
authors.initials: J
authors.lastname: Liu
authors.forename: Yingcai
authors.initials: Y
authors.lastname: Wang
authors.forename: Ying
authors.initials: Y
authors.lastname: Sun
authors.forename: Derek
authors.initials: D
authors.lastname: Marshall
authors.forename: Shichang
authors.initials: S
authors.lastname: Miao
authors.forename: George
authors.initials: G
authors.lastname: Tonn
authors.forename: Penny
authors.initials: P
authors.lastname: Anders
authors.forename: Joel
authors.initials: J
authors.lastname: Tocker
authors.forename: H Lucy
authors.initials: HL
authors.lastname: Tang
authors.forename: Julio
authors.initials: J
authors.lastname: Medina
mesh_terms: D018926:Anti-Allergic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D002460:Cell Line; D048430:Cell Shape / Q000187:drug effects; D055808:Drug Discovery; D004804:Eosinophils / Q000187:drug effects / Q000276:immunology; D006801:Humans; D011804:Quinolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*
chemical_list: D018926:Anti-Allergic Agents; D011804:Quinolines; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C542964:1,2,3,4-tetrahydroquinoline; C036293:prostaglandin D2 receptor