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Advancements in drug design have resulted in resurging interest in drugs that form covalent bonds with their targets, often referred to as targeted covalent inhibitors. Covalent drugs have the potential to provide enhanced potency and prolonged duration of action compared to non-covalent drugs. However, it is critical for covalent inhibitors to exhibit sufficient selectivity to mitigate off-target effects caused by binding to unintended proteins.

In this GEN webinar, our speakers will introduce innovative approaches to screen for covalent binders, including the use of covalent DNA-encoded libraries (DELs), high throughput screening library collections, and covalent fragment libraries for fragment-based hit generation. They will discuss synthetic strategies of covalent warheads, the unique DMPK properties of covalent drugs, and well-established assays to better characterize these molecules to support lead optimization efforts. Our speakers will also provide a comprehensive perspective on strategies and approaches that are crucial for accelerating research focused on covalent drug discovery. During the webinar, you’ll learn:

• Research strategies for discovering targeted covalent inhibitors

• Innovative technologies to synthesize and identify targeted covalent inhibitors

• DMPK properties and supporting assays for the lead optimization of targeted covalent inhibitors

A live Q&A session will follow the presentation, offering you a chance to pose questions to our expert panelists.