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(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
Authors:Bamford Mark J  Bailey Nicholas  Davies Susannah  Dean David K  Francis Leann  Panchal Terence A  Parr Christopher A  Sehmi Sanjeet  Steadman Jon G  Takle Andrew K  Townsend James T  Wilson David M
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
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.
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