Is your target a hit?
The cornerstone of the CETSA® method is the fact that a protein bound to a ligand has a different thermal stability than the unbound protein. CETSA® principles are then combined with LC-MS/ MS protein quantification to measure the selectivity of compounds by assessing thousands of proteins in parallel. It allows researchers to determine the impact on both individual proteins and entire pathways targeted by bioactive molecules. When performed in whole cell experiments, CETSA® Explore can also provide an analysis of a compound’s mechanism of action in a disease-relevant setting.
Unbiased proteome-wide assessment of compound selectivity
- CETSA® Explore is a versatile tool to address challenges throughout the drug discovery pipeline. The method can be applied to any cell and tissue, enabling a label-free assessment of a compound on up to 6000 proteins in a physiologically relevant matrix.
- Unbiased proteome-wide profiling makes CETSA® Explore uniquely positioned to help avoid failures in clinical development, by identifying issues with selectivity earlier in the process.
How can I confirm my target? Download our CETSA® Explore application note.
Publications
- Savitski et al. Science 2014
- Hendricks et al. ACS Chem Bio