Biological Relevance
Real biology,
real relevance
What you see in cells you’re
likely to see in patients
In drug discovery, preclinical target engagement studies should accurately reflect therapeutic effects in patients. CETSA ensures that proof of cellular target engagement—the direct interaction between a drug and its protein target—occurs in a physiologically relevant environment, significantly increasing the likelihood of success in drug discovery.
A drug’s pharmacological effect depends on the extent of its target engagement, while off-target interactions often drive toxicity and side effects. Therefore, a precise and reliable assessment of target engagement is critical for optimizing drug efficacy and minimizing risks.
What makes CETSA different
Traditional biochemical assays often fail to replicate real-world conditions because they rely on:
- Engineered cellular systems, which may not fully reflect native protein interactions.
- Tagged or truncated proteins, which can alter natural binding properties.
- Highly defined buffers, which do not mimic the complex cellular environment.
- Modified compounds may not behave like native drugs in biological systems.
In contrast, CETSA directly measures drug-target interactions in endogenous proteins, within intact cells and complex biological samples. This ensures that observed target engagement correlates with real biological effects, improving translation from preclinical research to clinical success.
Our services
We provide biologically relevant, high-quality, actionable data so you can make decisions with confidence.
See CETSA in action
Explore our case stories and discover how using CETSA can help you move your project forward.
Unlocking Challenging Targets with CETSA® Across Drug Discovery
Drug discovery increasingly focuses on targets that are difficult to address using traditional approaches. CETSA® enables direct measurement of target engagement in intact cells and complex biological …
Engaged but not degraded
Target engagement profiling of degrader compounds with CETSA CETSA® (Cellular Thermal Shift Assay) is a label-free method for studying small molecule-protein interactions and is especially useful in ta…
On Target Driven Efficacy Assessment of CDK2 Inhibitors in the Right Biological Context
Target Engagement and Selectivity Profiling in K562 and MCF7 Cells CETSA® is a label-free method for assessing target engagement of small molecule-protein interactions. Target engagement determination …