CETSA^® Explore – a mass spectrometry approach for target deconvolution and compound profiling

Phenotypic drug discovery recently regained popularity owing to its potential for delivering first-in-class treatments for diseases with unmet clinical needs. However, one of the major challenges to phenotypic approaches is the need for target deconvolution and hit confirmation.

CETSA^® (Cellular Thermal Shift Assay) Explore is an unbiased mass spectrometry-based, proteome-wide target engagement assessment method for compound profiling measuring not only direct binding but also subsequent downstream pathway events without any label in physiologically relevant conditions.

Helena Almqvist, Project Advisor at Pelago Bioscience will introduce the CETSA^® Explore method and also present different applications highlighting how this assay can guide and provide new insights at various stages of drug discovery.

Gizem Akçay, Head of Chemical Biology, Bayer Research and Innovation Center will present how CETSA^® Explore was part of a target deconvolution effort following a phenotypic screen. The results were further validated using a targeted CETSA^® approach to confirm direct binding.

Key learning objectives

• Advantages of assessing target engagement in physiological conditions, without protein or compound modifications.
• What is CETSA^® Explore, an unbiased proteome-wide target engagement assay and how it can accelerate drug discovery programs.
• CETSA^® Explore application for target deconvolution and target identification.
• Understanding compound selectivity and Mechanism of Action with CETSA^® Explore.
• How CETSA^® Navigate – a target CETSA® format can be used for further target engagement validation.

Who should attend?

• Drug discovery researchers
• Chemical biologists
• Scientists working in early drug development, phenotypic screens, and target deconvolution projects.

Certificate of attendance
All webinar participants can request a certificate of attendance, including a learning outcomes summary, for continuing education purposes.