Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification

Tom D Heightman; Jackie S Scott; Mark Longley; Vincent Bordas; David K Dean; Richard Elliott; Gail Hutley; Jason Witherington; Lee Abberley; Barry Passingham; Manuela Berlanga; Maite de Los Frailes; Alan Wise; Ben Powney; Alison Muir; Fiona McKay; Sharon Butler; Kim Winborn; Christopher Gardner; Jill Darton; Colin Campbell; Gareth Sanger

doi:10.1016/j.bmcl.2007.09.067

Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6584-7. doi: 10.1016/j.bmcl.2007.09.067. Epub 2007 Sep 25.

Affiliation

¹ 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. [email protected]

PMID: 17942309
DOI: 10.1016/j.bmcl.2007.09.067

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.

Publication types

Comparative Study

MeSH terms

Animals
Gastric Emptying / drug effects
Gastric Emptying / physiology
Human Growth Hormone / agonists
Humans
Indoles / chemistry*
Indoles / pharmacology
Rats
Receptors, Ghrelin / agonists*
Receptors, Ghrelin / physiology
Stereoisomerism

Substances

Indoles
Receptors, Ghrelin
Human Growth Hormone
indoline