Darren Jason Mitchell

TL;DR: In this paper, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine is described, where R1, R2, R3, P, X, Y, q, r ans s are as defined in the specification.

TL;DR: This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.

TL;DR: The discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain are reported.

TL;DR: The discovery of a hit from a fragment-based targeted array is described, which produced the first known micromolar inhibitors of the ATAD2 bromodomain.

TL;DR: This work reports the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2, a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class.