This presentation will entail an overview of encoded library technology (ELT) from the inception of the technology to current integration into one of the hit/lead identification platforms at GlaxoSmithKline (GSK). We will disclose some milestones during the platform development journey including technical advances in library chemistry, selection methodology, data analysis, and off-DNA decision making and hit confirmation for a number of chemical series. One of the recent developments in the use of ELT is efficient and rapid assessment of chemical tractability of multiple target proteins in parallel, a major hurdle in drug discovery. We have established a new paradigm to allow for rapid prioritization and streamlining of target proteins based on their ligandability prior to heavy investment in early stage therapeutic targets. We will disclose several examples of this panel screening approach and its output including hit/lead series for each tractability panel as a proof of concept of paradigm output.

Efficient discovery of lead molecules for hundreds of target proteins in parallel via DNA encoded chemical library: A platform for prioritizing therapeutic targets in a single experiment

252nd National Meeting (2016)

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