title: (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
abstract: The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases.
authors.affiliation: GlaxoSmithKline Pharmaceuticals, Neurology & GI Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Mark_J_Bamford@GSK.com
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Bamford
authors.forename: Nicholas
authors.initials: N
authors.lastname: Bailey
authors.forename: Susannah
authors.initials: S
authors.lastname: Davies
authors.forename: David K
authors.initials: DK
authors.lastname: Dean
authors.forename: Leann
authors.initials: L
authors.lastname: Francis
authors.forename: Terence A
authors.initials: TA
authors.lastname: Panchal
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Parr
authors.forename: Sanjeet
authors.initials: S
authors.lastname: Sehmi
authors.forename: Jon G
authors.initials: JG
authors.lastname: Steadman
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Takle
authors.forename: James T
authors.initials: JT
authors.lastname: Townsend
authors.forename: David M
authors.initials: DM
authors.lastname: Wilson
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D038744:Ribosomal Protein S6 Kinases, 90-kDa / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D004791:Enzyme Inhibitors; D007093:Imidazoles; D010069:Oxadiazoles; D011725:Pyridines; D038744:Ribosomal Protein S6 Kinases, 90-kDa; C116919:mitogen and stress-activated protein kinase 1