AACR POSTER – Selectivity

Unbiased Selectivity Profiling with CETSA® and Mass Spectrometry

Unbiased Selectivity Profiling: Revealing True Compound Specificity and Off-Target Interactions

In drug discovery, ensuring selectivity and minimizing off-target effects are crucial for improving the safety and efficacy of therapeutic compounds. Pelago Bioscience’s Selectivity Profiling Service, powered by CETSA (Cellular Thermal Shift Assay) coupled with mass spectrometry, offers a comprehensive, unbiased approach to assess compound interactions across over 5,000 proteins. This innovative service enables precise identification of both on-target and off-target proteins, including those often missed by conventional screening panels.

Our service provides a clear understanding of compound selectivity and potency, helping researchers prioritize lead compounds early in the discovery process and avoid potential liabilities. By profiling well-known probes and marketed drugs, such as Abemaciclib and Palbociclib, we demonstrate how unbiased profiling reveals key off-target interactions and highlights the need for early identification of promiscuous compounds. This approach ensures that selectivity profiling is comprehensive, reproducible, and scalable, supporting informed decision-making for the advancement of drug candidates.

Explore how our CETSA-based Selectivity Profiling can help refine your drug discovery efforts and optimize lead selection.