title: The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
abstract: Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists.
authors.affiliation: Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG12NY, UK. james.m.bailey@gsk.com
authors.forename: James M
authors.initials: JM
authors.lastname: Bailey
authors.forename: Jackie S
authors.initials: JS
authors.lastname: Scott
authors.forename: Jonathan B
authors.initials: JB
authors.lastname: Basilla
authors.forename: Victoria J
authors.initials: VJ
authors.lastname: Bolton
authors.forename: Izzy
authors.initials: I
authors.lastname: Boyfield
authors.forename: David G
authors.initials: DG
authors.lastname: Evans
authors.forename: Etienne
authors.initials: E
authors.lastname: Fleury
authors.forename: Tom D
authors.initials: TD
authors.lastname: Heightman
authors.forename: Emma M
authors.initials: EM
authors.lastname: Jarvie
authors.forename: Kirk
authors.initials: K
authors.lastname: Lawless
authors.forename: Kim L
authors.initials: KL
authors.lastname: Matthews
authors.forename: Fiona
authors.initials: F
authors.lastname: McKay
authors.forename: Hindy
authors.initials: H
authors.lastname: Mok
authors.forename: Alison
authors.initials: A
authors.lastname: Muir
authors.forename: Barry S
authors.initials: BS
authors.lastname: Orlek
authors.forename: Gareth J
authors.initials: GJ
authors.lastname: Sanger
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Stemp
authors.forename: Alexander J
authors.initials: AJ
authors.lastname: Stevens
authors.forename: Mervyn
authors.initials: M
authors.lastname: Thompson
authors.forename: John
authors.initials: J
authors.lastname: Ward
authors.forename: Kalindi
authors.initials: K
authors.lastname: Vaidya
authors.forename: Susan M
authors.initials: SM
authors.lastname: Westaway
mesh_terms: D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D002626:Chemistry, Pharmaceutical; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D055808:Drug Discovery; D008956:Models, Chemical; D015394:Molecular Structure; D011964:Receptors, Gastrointestinal Hormone / Q000819:agonists*; D018013:Receptors, Neuropeptide / Q000819:agonists*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*; D013450:Sulfones / Q000494:pharmacology*
chemical_list: D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; D013449:Sulfonamides; D013450:Sulfones; C050802:motilin receptor