Paul Bamborough

TL;DR: The biphenyl amides (BPAs) are a novel series of p38alpha MAP kinase inhibitor and the optimisation of the series to give compounds that are potent in an in vivo disease model is discussed.

TL;DR: 5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors and their optimization to yield compounds with cell activity and brain permeability is described.

TL;DR: The in-vitro and cellular activity profile of GSK789, a potent, cell permeable and highly selective inhibitor of the first bromodomains of the BET family of proteins is disclosed.

TL;DR: In this article, a selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was described, and the optimization of this series leading to the identification of a superior BRPF 1 inhibitor suitable for in vivo studies.

TL;DR: In this article, the identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole-thiophene carbonitrile inhibitors of IKK-e kinase is described.