title: Identification of small molecule agonists of the motilin receptor.
abstract: High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to target 7-transmembrane (7-TM) receptors. Further investigation of the structure-activity relationship within the series resulted in the identification of compound (22) as a potent and selective agonist at the motilin receptor.
authors.affiliation: Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. tom.heightman@sgc.ox.ac.uk
authors.forename: Tom D
authors.initials: TD
authors.lastname: Heightman
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Conway
authors.forename: David F
authors.initials: DF
authors.lastname: Corbett
authors.forename: Gregor J
authors.initials: GJ
authors.lastname: Macdonald
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Stemp
authors.forename: Susan M
authors.initials: SM
authors.lastname: Westaway
authors.forename: Paolo
authors.initials: P
authors.lastname: Celestini
authors.forename: Stefania
authors.initials: S
authors.lastname: Gagliardi
authors.forename: Mauro
authors.initials: M
authors.lastname: Riccaboni
authors.forename: Silvano
authors.initials: S
authors.lastname: Ronzoni
authors.forename: Kalindi
authors.initials: K
authors.lastname: Vaidya
authors.forename: Sharon
authors.initials: S
authors.lastname: Butler
authors.forename: Fiona
authors.initials: F
authors.lastname: McKay
authors.forename: Alison
authors.initials: A
authors.lastname: Muir
authors.forename: Ben
authors.initials: B
authors.lastname: Powney
authors.forename: Kim
authors.initials: K
authors.lastname: Winborn
authors.forename: Alan
authors.initials: A
authors.lastname: Wise
authors.forename: Emma M
authors.initials: EM
authors.lastname: Jarvie
authors.forename: Gareth J
authors.initials: GJ
authors.lastname: Sanger
mesh_terms: D000818:Animals; D001665:Binding Sites; D002462:Cell Membrane / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008956:Models, Chemical; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism; D011964:Receptors, Gastrointestinal Hormone / Q000819:agonists* / Q000737:chemistry*; D018013:Receptors, Neuropeptide / Q000819:agonists* / Q000737:chemistry*; D011994:Recombinant Proteins / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D043562:Receptors, G-Protein-Coupled; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; D011994:Recombinant Proteins; C050802:motilin receptor