title: The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.
abstract: A novel small molecule NPY Y2 antagonist (3) identified from high throughput screening is described. A subsequent SAR study and optimisation programme based around this molecule is also described, leading to the identification of potent and soluble pyridyl analogue 36.
authors: GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
authors: Gillian E
authors: GE
authors: Lunniss
authors: Ashley A
authors: AA
authors: Barnes
authors: Nick
authors: N
authors: Barton
authors: Matteo
authors: M
authors: Biagetti
authors: Federica
authors: F
authors: Bianchi
authors: Stephen M
authors: SM
authors: Blowers
authors: Laura
authors: L
authors: Caberlotto
authors: Amanda
authors: A
authors: Emmons
authors: Ian P
authors: IP
authors: Holmes
authors: Dino
authors: D
authors: Montanari
authors: Ros
authors: R
authors: Norris
authors: Dewi J
authors: DJ
authors: Walters
authors: Steve P
authors: SP
authors: Watson
mesh_terms: D000577:Amides / Q000737:chemistry*; D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives* / Q000494:pharmacology; D001552:Benzazepines / Q000494:pharmacology*; D002625:Chemistry, Organic / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D010446:Peptide Fragments / Q000737:chemistry; D011485:Protein Binding; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D001552:Benzazepines; D010446:Peptide Fragments; D017476:Receptors, Neuropeptide Y; C095889:neuropeptide Y2 receptor; D001120:Arginine; C403256:BIIE 0246