Drug discovery teams face persistent obstacles when tackling targets that defy traditional small-molecule approaches. Flat protein-protein interaction (PPI) surfaces, shallow or dynamic binding pockets, and unsuccessful HTS campaigns often produce weak or unprogressable hits. For organizations pursuing novel targets or molecular glues, selecting a suboptimal strategy can waste time, budget, and momentum.
This webinar will present practical strategies to address these challenges, emphasizing how to align a discovery campaign with the screening method(s) most likely to deliver tractable results. You will learn how to assess target space, pair suitable screening routes, and design discovery campaigns that maximise success potential. We will focus on fragment-based, covalent compound, and DNA-encoded library approaches, coupled with chemistry strategies to select and quickly progress genuine, high-quality hits.
Our experts will illustrate how covalent compounds can enable both disruption and stabilization of PPIs, including applications in molecular glue discovery. We will show how exquisite cooperativity can be achieved, along with practical guidance on distinguishing true hits from artefacts and improving hit quality.
If you are working with difficult targets, stalled programs, or exploring molecular glue opportunities, this session will provide clear, actionable strategies to identify and progress true hits. Register today to learn how to turn resistant targets into tractable opportunities.
Key Learning Objectives
- Identify key challenges that make certain biological targets resistant to traditional small-molecule approaches.
- Compare conventional screening methods with covalent, fragment-based, and DEL strategies.
- Evaluate when to apply covalent approaches in PPI and molecular glue campaigns.
- Apply best practices to improve hit quality and reduce artefacts in early discovery campaigns.
