Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
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.
Heightman
Tom D
TD
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
Scott
Jackie S
JS
Longley
Mark
M
Bordas
Vincent
V
Dean
David K
DK
Elliott
Richard
R
Hutley
Gail
G
Witherington
Jason
J
Abberley
Lee
L
Passingham
Barry
B
Berlanga
Manuela
M
de Los Frailes
Maite
M
Wise
Alan
A
Powney
Ben
B
Muir
Alison
A
McKay
Fiona
F
Butler
Sharon
S
Winborn
Kim
K
Gardner
Christopher
C
Darton
Jill
J
Campbell
Colin
C
Sanger
Gareth
G
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
D007211:Indoles; D054440:Receptors, Ghrelin; D019382:Human Growth Hormone; C057812:indoline