2. Academic Validation
  3. Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate

Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate

  • J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q.
Susan M Westaway 1,  Samantha L Brown,  Stephen C M Fell,  Christopher N Johnson,  David T MacPherson,  Darren J Mitchell,  James W Myatt,  Steven J Stanway,  Jon T Seal,  Geoffrey Stemp,  Mervyn Thompson,  Kirk Lawless,  Fiona McKay,  Alison I Muir,  Jonathan M Barford,  Chermaine Cluff,  Sadhia R Mahmood,  Kim L Matthews,  Shiyam Mohamed,  Beverley Smith,  Alexander J Stevens,  Victoria J Bolton,  Emma M Jarvie,  Gareth J Sanger
Affiliations

Affiliation

  • 1 Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts, SG1 2NY, UK. sue.m.westaway@gsk.com
PMID: 19191554 DOI: 10.1021/jm801332q
Abstract

N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule Motilin Receptor Agonist. It possesses excellent activity at the recombinant human Motilin Receptor and also at the native rabbit Motilin Receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.

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