Like a fish out of water proteins out of the cells are not in their natural environment and their behaviour will be compromised.
Exploring your proteins out of the cell?
Refers to something being completely out of place
So, is your compound really therapeutic?
– CETSA can tell.
At target identification – at lead generation – at lead optimization – at your choice. We support all stages of drug discovery. CETSA offers highly accurate assessment of target engagement in an authentic cell environment. No protein modification. No ligand modification. Just physiological conditions. Because you can learn a lot from a fish out of water, but you’ll never see it swim.
This is CETSA®
Thermal shift assays (TSAs) are a well-established techniques for measuring ligand binding to purified proteins. They involve subjecting the protein to varying temperatures and quantifying its thermal denaturation. The key principle is that when a ligand is bound to a protein, the melting is altered, which is known as a ‘thermal shift’ and can be used to quantify the affinity of the ligand-protein interaction.
”Perhaps the most important unique benefit of using CETSA® during lead generation is that it allows you to directly discard false positives, allowing you to fail faster and prioritize only the very best compounds”
Stina Lundgren, Drug Discovery Expert
CETSA® (Cellular Thermal Shift Assay) is based on this fundamental principle but leverages the novel insight that the melt curves can be generated in intact cells and tissues.
Adopting CETSA early can reduce your project timeline by 6-12 months and expedite the progress of projects from lead generation into the lead optimization stage.
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The Home of CETSA®
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Want to learn more
- CETSA: Navigate your Chemistry and Explore the Biology to Enhance your Drug Discovery Project
In this eBook, we outline:
• Why CETSA is the best way to measure target engagement
• How you can implement CETSA during lead generation and lead optimization to drive the development of the right compounds and get the most value out of your drug discovery projects - Right tools, right time: Adopting CETSA ® MS earlier in target identification can boost your drug discovery success
In this eBook, we outline:
• How implementing mass spectrometry-based proteomics tools earlier can boost drug discovery success
• We discuss the two main MS-based proteomics methods you can use in your target identification studies, and why choosing the most efficient and reliable tool from the earliest stage is vital for the long-term success of your research.
