Lisa Elkin

TL;DR: The bile salt export pump (BSEP) is located on the canalicular plasma membrane of hepatocytes and plays an important role in the biliary clearance of bile acids (BAs), so screening compounds in a discovery setting or conducting mechanistic studies to address clinical findings must consider the direct (inhibitory) effect of the parent drug and metabolites on multiple BA transporters.

TL;DR: The results support a model where the pseudokinase domain regulates activation of the catalytic domain by forming receptor-regulated inhibitory interactions, and represent a novel approach to the design of potent and selective agents for the treatment of autoimmunity.

TL;DR: A novel series of imidazo[1,2-a]pyrazine diarylureas that show nanomolar potency for the EphB4 receptor, in addition to potent activity against several other RTKs are reported.

TL;DR: Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.

TL;DR: The infrastructure developed and applied at Bristol-Myers Squibb for 1536-well high content screening is outlined and key lessons learned are discussed, including how to interpret the large volumes of content-rich information generated.