Your key to biological relevance

What you study in cells, you will also 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 development. 

A drug’s pharmacological effect depends on the extent of its target engagement, while off-target interactions often drive toxicity and side effects. Therefore, from early hit identification to preclinical and clinical development, a precise and reliable assessment of target engagement is critical for optimizing drug efficacy and minimizing risks. 

Why CETSA Offers a Superior Approach 

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. 

Unlock the Full Potential of CETSA in Your Research 

Pelago Bioscience is the leading provider of CETSA technology, offering expert-driven solutions for target engagement studies at every stage of drug discovery. 

• Want to learn how CETSA can enhance your drug development strategy? 

• Looking for tailored CETSA solutions for your research? 

Contact Pelago Bioscience today to discuss how CETSA can help advance your drug discovery pipeline with confidence.