title: Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
abstract: High throughput screening combined with efficient datamining and parallel synthesis led to the discovery of a novel series of indolines showing potent in vitro ghrelin receptor agonist activity and acceleration of gastric emptying in rats.
authors.affiliation: Department of Medicinal Chemistry & DMPK, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Tom.D.Heightman@gsk.com
authors.forename: Tom D
authors.initials: TD
authors.lastname: Heightman
authors.forename: Jackie S
authors.initials: JS
authors.lastname: Scott
authors.forename: Mark
authors.initials: M
authors.lastname: Longley
authors.forename: Vincent
authors.initials: V
authors.lastname: Bordas
authors.forename: David K
authors.initials: DK
authors.lastname: Dean
authors.forename: Richard
authors.initials: R
authors.lastname: Elliott
authors.forename: Gail
authors.initials: G
authors.lastname: Hutley
authors.forename: Jason
authors.initials: J
authors.lastname: Witherington
authors.forename: Lee
authors.initials: L
authors.lastname: Abberley
authors.forename: Barry
authors.initials: B
authors.lastname: Passingham
authors.forename: Manuela
authors.initials: M
authors.lastname: Berlanga
authors.forename: Maite
authors.initials: M
authors.lastname: de Los Frailes
authors.forename: Alan
authors.initials: A
authors.lastname: Wise
authors.forename: Ben
authors.initials: B
authors.lastname: Powney
authors.forename: Alison
authors.initials: A
authors.lastname: Muir
authors.forename: Fiona
authors.initials: F
authors.lastname: McKay
authors.forename: Sharon
authors.initials: S
authors.lastname: Butler
authors.forename: Kim
authors.initials: K
authors.lastname: Winborn
authors.forename: Christopher
authors.initials: C
authors.lastname: Gardner
authors.forename: Jill
authors.initials: J
authors.lastname: Darton
authors.forename: Colin
authors.initials: C
authors.lastname: Campbell
authors.forename: Gareth
authors.initials: G
authors.lastname: Sanger
mesh_terms: D000818:Animals; D005746:Gastric Emptying / Q000187:drug effects / Q000502:physiology; D019382:Human Growth Hormone / Q000819:agonists; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D054440:Receptors, Ghrelin / Q000819:agonists* / Q000502:physiology; D013237:Stereoisomerism
chemical_list: D007211:Indoles; D054440:Receptors, Ghrelin; D019382:Human Growth Hormone; C057812:indoline