EMBL Course: Target Engagement in Biology and Drug Discovery

Small molecules play an important role in biological research and drug discovery. Demonstrating target engagement by a small molecule is essential to understand its mechanism of action. This course will give a solid practical and theoretical grounding in evaluating how a small molecule interacts with its biological target in cells or in vitro, and its role in drug discovery. This course will use proteins of the kinase family to exemplify the general principles and methodologies and their application.

Topics: Cellular Thermal Shift Assay (CETSA), Bioluminescence Resonance Energy Transfer (BRET), PROTAC: targeted protein degradation, Computational methods for target identification