title: Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
abstract: Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.
authors.affiliation: Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. adrian.2.hall@gsk.com
authors.forename: Adrian
authors.initials: A
authors.lastname: Hall
authors.forename: Stephen
authors.initials: S
authors.lastname: Atkinson
authors.forename: Susan H
authors.initials: SH
authors.lastname: Brown
authors.forename: Iain P
authors.initials: IP
authors.lastname: Chessell
authors.forename: Anita
authors.initials: A
authors.lastname: Chowdhury
authors.forename: Gerard M P
authors.initials: GM
authors.lastname: Giblin
authors.forename: Paul
authors.initials: P
authors.lastname: Goldsmith
authors.forename: Mark P
authors.initials: MP
authors.lastname: Healy
authors.forename: Karamjit S
authors.initials: KS
authors.lastname: Jandu
authors.forename: Matthew R
authors.initials: MR
authors.lastname: Johnson
authors.forename: Anton D
authors.initials: AD
authors.lastname: Michel
authors.forename: Alan
authors.initials: A
authors.lastname: Naylor
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Sweeting
mesh_terms: D006801:Humans; D020128:Inhibitory Concentration 50; D011485:Protein Binding; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology*; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
chemical_list: C545635:PTGER1 protein, human; D011758:Pyrroles; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype