Drug Discovery 2024 – ELRIG UK

Poster session

Poster 2 Title: Deep characterization of binding kinetics for 210kinase inhibitors against 80+ kinases

Presenter: Jonathan Popplewell, PhD, Field Applications Scientist, Carterra

Abstract: As a drug target class, kinases continue to provide a wealth of opportunities for addressing human disease, but often can be challenging to work with in vitro. Additionally, the ubiquitous nature of kinases across many critical pathways means therapeutic targeting this class necessitates careful consideration regarding off-target profiles. Here we highlight the power of combining an extensive panel of active kinases with HT-SPR to generate a wealth of compound binding information. Over 80,000 binding interactions were measured during a 3-day label-free screen. Detailed kinetics were then subsequently obtained for hits of interest. Beyond simple yes/no reporting, this approach allows for nuanced kinetic profiling for up to hundreds of binding events in parallel enabling thoughtful discovery of safe and efficacious drug candidates.

Poster 2 Title: Large-Scale Characterization of Drug Candidates Against Transmembrane Receptors Using HT-SPR

Presenter: Andrew Goodhead, Sales Executive, Carterra

Abstract: Membrane targets make up a substantial part of the overall “undruggable” therapeutic space that has recently garnered widespread interest. Despite encouraging improvements in the tools to screen for therapeutics against membrane-bound targets, there are still many practical limitations owing to the challenges of working with proteins that are not highly stable outside of the cellmembrane environment. High-throughput surface plasmon resonance (HT-SPR) is a powerful technique that is transforming characterization workflows and enabling a greater breadth and depth of information for drug candidates. Here we demonstrate the ability to quantitatively assess binding kinetics for panels of antibodies against membrane receptors in several formats. This workflow highlights opportunities to perform detailed binding characterization for up to thousands of drug candidates in parallel.