Christopher Dimitri, PhD
NCE Molecular Discovery - GlaxoSmithKline, Massachusetts, United States
Recent advances in both genome-wide screening and genome-wide analyses, e.g. genome-wide CRISPR screens and GWAS, respectively, have enabled the identification of numerous putative therapeutically relevant targets for hit identification programs. Pursuing all of these targets in small molecule hit ID programs is neither feasible nor warranted.
At GSK, we have integrated both in silico and experimental methods to rapidly predict the small molecule tractability of novel targets. Specifically, we have deployed the Encoded Library Technology (ELT) & Affinity Selection Mass Spectrometry (ASMS) platforms to conduct experimental Tractability Assessments (eTA). Together, these outcomes allow us to quickly prioritize novel therapeutically relevant targets based on empirical data and focus small molecule hit identification efforts on those that are most likely to succeed. A recent tractability project will be shared as a case study demonstrating the impact of our approaches.