(1153-B) Discovery and Development of Small Molecules by Information-rich Next Generation Multiplexing SPR
Monday, February 5, 2024
2:00 PM – 3:00 PM EST
Location: Exhibit Halls AB
Abstract: Surface Plasmon Resonance is an established and widely used biophysical technology in screening and lead development campaigns for novel drug candidates. The real-time, label-free analysis of interactions offers additional insights into kinetics. Multiplexing SPR systems further allow to study the interaction of a drug candidate against multiple targets simultaneously. We developed a novel microfluidic set-up that allows to determine affinity, selectivity and thermodynamic constants in a single assay at high throughput. Partnered with our established SPR+ detection system for state-of-the-art sensitivity, the instrument provides multiple assay formats perfectly suited for small molecule discovery and development. We present data from the novel microfluidic set-up proving performance and robustness. Affinity determination and selectivity is showcased with a compound set against two bacterial glutaminyl cyclases. The flow cell design offers the concept of “extended screener”, a technical feature enabling extended capabilities for long screening runs and cases of loss in activity of the relevant protein. Finally, we assessed the capability of the instrument for the determination of thermodynamic constants for a well-established small molecule-protein interaction. We herewith present an SPR microfluidic set-up with industry-leading throughput in affinity determination and multiplexing capabilities for all types of analytes. Thus, the extension of typical parameters from a SPR experiment by a quantitative selectivity assessment allows for a more informed hit selection process in screening campaigns.