See on- and off-target activity across the proteome

Selectivity profiling using CETSA offers a rapid and unbiased approach to understanding how compound activity is distributed across proteins beyond the intended target. The focus is on identifying on-target engagement alongside secondary and off-target interactions early, before selectivity issues become limiting for chemistry or progression decisions.

The service is designed for high-throughput selectivity assessment using standard cell lysate, enabling rapid profiling of compound–protein interactions across a broad protein space. By avoiding predefined target panels, this unbiased approach captures both expected and unexpected interactions, helping reveal liabilities and opportunities that may not be apparent with narrower methods.

CETSA, combined with quantitative mass spectrometry, provides unbiased measurement of compound–protein interactions with short turnaround times. The resulting selectivity profiles provide clear, actionable insights into target engagement and secondary pharmacology, supporting chemistry optimization and enabling teams to address selectivity risks quickly and efficiently.

The path of a Selectivity Profiling project

A quick look at how it works

Start-Up

– Compound submission

Submit your compounds to us and our team will work with you to answer any questions you may have.

Processing

– We do the work

We use well established workflows and state-of-the-art equipment to perform the project. Once data is generated, we apply standardized processing and analysis pipelines to ensure accurate, consistent, and high-quality results.

Insights

– Result report

When the analysis is complete, we share the results with you and guide you through the key findings.

Let’s talk

For us, every project is a partnership.
Send us a message or book a free scoping call with one of our experts.

Let’s collaborate

Unbiased Selectivity Profiling with CETSA® and Mass Spectrometry

CETSA mass spectrometry profiling enables unbiased analysis of compound selectivity in drug discovery—helping reduce off-target effects, improve safety, and accelerate informed decision-making. This technique combines the power of CETSA® (Cellular Thermal Shift Assay) with quantitative mass spectrometry to identify how compounds interact with thousands of proteins in physiologically relevant systems.

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What Is Unbiased Selectivity Profiling? A CETSA®-Based Approach

While selectivity—the ability of a compound to modulate its primary target with minimal interaction with non-target proteins—has long been a pharmacological ideal, the methodologies used to evaluate it are undergoing a paradigm shift. At Pelago Bioscience, we advocate for a more integrative, data-driven approach: unbiased selectivity profiling with CETSA®.

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