title: Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
abstract: Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists.
authors.affiliation: Department of Pharmaceutical Development, Physical Properties and Developability, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
authors.forename: David L
authors.initials: DL
authors.lastname: Carlton
authors.forename: Lissa J
authors.initials: LJ
authors.lastname: Collin-Smith
authors.forename: Alejandro J
authors.initials: AJ
authors.lastname: Daniels
authors.forename: David N
authors.initials: DN
authors.lastname: Deaton
authors.forename: Aaron S
authors.initials: AS
authors.lastname: Goetz
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Laudeman
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Littleton
authors.forename: David L
authors.initials: DL
authors.lastname: Musso
authors.forename: Ronda J Ott
authors.initials: RJ
authors.lastname: Morgan
authors.forename: Jerzy R
authors.initials: JR
authors.lastname: Szewczyk
authors.forename: Cunyu
authors.initials: C
authors.lastname: Zhang
mesh_terms: D016367:Baculoviridae / Q000378:metabolism; D001562:Benzimidazoles / Q000737:chemistry; D001921:Brain / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005617:Chlorofluorocarbons, Methane / Q000737:chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007700:Kinetics; D008956:Models, Chemical; D009853:Omeprazole / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry; D018004:Receptors, Bombesin / Q000819:agonists* / Q000737:chemistry; D013440:Sulfides / Q000737:chemistry
chemical_list: D001562:Benzimidazoles; D005617:Chlorofluorocarbons, Methane; D011725:Pyridines; D018004:Receptors, Bombesin; D013440:Sulfides; C107120:bombesin receptor subtype 3; C031000:benzimidazole; D009853:Omeprazole; C009554:fluoroform