title: The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.
abstract: A novel pyrrole-2-carboxamide series of p38alpha inhibitors, discovered through the application of virtual screening, is presented. Following evaluation of activity, selectivity and developability properties of commercially available analogues, a synthesis program enabled rapid assessment of the series' suitability for further lead optimisation studies.
authors.affiliation: GlaxoSmithKline R&D, Medicines Research Centre, Stevenage, Hertfordshire, UK. kenneth.d.down@gsk.com
authors.forename: Kenneth
authors.initials: K
authors.lastname: Down
authors.forename: Paul
authors.initials: P
authors.lastname: Bamborough
authors.forename: Catherine
authors.initials: C
authors.lastname: Alder
authors.forename: Amanda
authors.initials: A
authors.lastname: Campbell
authors.forename: John A
authors.initials: JA
authors.lastname: Christopher
authors.forename: Maria
authors.initials: M
authors.lastname: Gerelle
authors.forename: Steve
authors.initials: S
authors.lastname: Ludbrook
authors.forename: Dave
authors.initials: D
authors.lastname: Mallett
authors.forename: Geoff
authors.initials: G
authors.lastname: Mellor
authors.forename: David D
authors.initials: DD
authors.lastname: Miller
authors.forename: Rosannah
authors.initials: R
authors.lastname: Pearson
authors.forename: Keith
authors.initials: K
authors.lastname: Ray
authors.forename: Yemisi
authors.initials: Y
authors.lastname: Solanke
authors.forename: Don
authors.initials: D
authors.lastname: Somers
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D057166:High-Throughput Screening Assays; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D048051:p38 Mitogen-Activated Protein Kinases