Bhumika Karamshi

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 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 study represents the first report of a demethylase high-content imaging assay with the ability to capture a repertoire of pharmacological tools, which are likely both to inform mechanistic understanding of how JMJD3 is modulated and to contribute to the identification of novel therapeutic modalities for this dem methylase enzyme.

TL;DR: These highly potent, selective, and orally active EP3 antagonists are excellent tool compounds for investigating and validating potential therapeutic benefits from selectively inhibiting the EP3 receptor.

TL;DR: The discovery of a new class of inhibitors by high-throughput screening and how the difficulties encountered in establishing a screening triage capable of finding progressible hits were overcome by data-driven optimization are described.