We understand that bringing a drug to market is costly and it’s important to have confidence in your compound drug throughout each step of the drug discovery process.
Cellular Thermal Shift assays (CETSA®), from Pelago Bioscience, together with PerkinElmer Alpha technology allows you to do just that. With CETSA® and Alpha you can check target engagement early in the drug discovery process, saving you time and money. Together these assays allow you to monitor binding of your compounds of interest in the natural living cellular environment, confirming whether your compounds interact with your target of interest or not. The ability to work in an unbiased and more physiologically relevant way means no molecular engineering is required, allows you to choose disease-relevant cell models, and overcomes limitations of biochemical assays. Alpha-CETSA® provides you with the confidence you need to proceed with potential compounds, and ultimately improves productivity and reduces failure rate.
CETSA® gives a quantitative measure of target engagement by assessing binding of the compounds to the target, which causes thermal stability upon heating. A thermal melting curve is prepared using known positive and negative controls identifying a certain temperature set point where compound-stabilized protein target stays in supernatant and non-compound binding leads to protein aggregation/precipitation. The compound-stabilized protein in solution is then detected by the well-established Alpha technology. Alpha technology is a no-wash, highly sensitive assay with a broad dynamic range, and fast time-to-results. This bead-based proximity assays enables the detection and screening of targets of interest in a reliable, high-throughput format.
The Alpha CETSA® product line brings together Pelago Bioscience’s CETSA® knowledge and PerkinElmer’s 20 years Alpha experience. More validated kits will be released, so check back regularly to see the latest list of targets available. If you do not find your target of interest on the current list, we are happy to work with you to turn your target into a validated kit.
For research use only. CETSA® is a registered trademark of Pelago Bioscience AB. Please note that a valid CETSA® subscription is required for kit use.
Alpha CETSA® Assay Principle. Principle of the CETSA® melting curve and thermal stabilization by compound binding used to assess target engagement early in the drug discovery process and Alpha assay use for detection.
For results in half the time of ELISA, without wash steps, and with excellent sensitivity in a variety of matrices, including serum and plasma.
The principle of detection of the soluble protein by the Alpha CETSA® assay is shown in the figure above. Only the soluble protein will lead to the generation of an Alpha signal (top), while the thermally denaturated insoluble protein does not generate the proximity needed for an Alpha signal (bottom).
For studying pathways or phosphorylated proteins in whole cells or studying endogenous receptors.
The principle of detection of the soluble protein by the Alpha SureFire CETSA® assay is shown in the figure above. Only the soluble protein will lead to the generation of an Alpha signal (top), while the thermally denaturated unsoluble protein is unable to create the proximity needed for the generation of an Alpha signal (bottom).
When it comes to developing assays or troubleshooting issues, always know you’re never on your own.
Whatever the assay you have in mind, you need the right technologies for your target. We can custom conjugate your antibody or biomolecule to any bead, or biotinylate or DIG-label your targets, so you can develop the assay you need. If you prefer, we can even perform the assay development for you.
FAS: Our global team of Field Application Scientists are hands-on subject matter experts in assay development. They are available to assist in both assay development and troubleshooting.
Application Support Knowledgebase (ASK): Need help at 1am? We’ve got it covered. The Application Support Knowledgebase (ASK) contains detailed information on assay development, protocols, tips, FAQs, citations, troubleshooting and more. Accessible 24 hours a day, 7 days a week on our website www.perkinelmer.com/AlphaCETSA/ASK
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Measure binding of small molecule drug candidates to target protein in a cellular environment with Alpha CETSA® target engagement assays. For use in combination with Pelago Bioscience's CETSA® (Cellular Thermal Shift Assay) technology, this kit provides a convenient no-wash assay for detection and quantitation of small molecule binding to target protein, and can be used in hit identification, hit confirmation, and lead optimization studies for increased confidence and better prediction early in the drug discovery process.
Please note that a valid CETSA® subscription from Pelago Biosciences is required for use.
Measure binding of small molecule drug candidates to target protein in a cellular environment with Alpha CETSA® target engagement assays. For use in combination with Pelago Bioscience's CETSA (Cellular Thermal Shift Assay) technology, this kit provides a convenient no-wash assay for detection and quantitation of small molecule binding to Cereblon, and can be used in hit identification, hit confirmation, and lead optimization studies for increased confidence and better prediction early in the drug discovery process. Please note that a valid CETSA subscription from Pelago Biosciences is required for use.
Measure binding of small molecule drug candidates to target protein in a cellular environment with Alpha SureFire® CETSA® target engagement assays. For use in combination with Pelago Bioscience's CETSA® (Cellular Thermal Shift Assay) technology, this kit provides a convenient no-wash assay for detection and quantitation of small molecule binding to CDK2, and can be used in hit identification, hit confirmation, and lead optimization studies for increased confidence and better prediction early in the drug discovery process. Please note that a valid CETSA® subscription from Pelago Biosciences is required for use.
Measure binding of small molecule drug candidates to target protein in a cellular environment with Alpha SureFire® CETSA® target engagement assays. For use in combination with Pelago Bioscience's CETSA® (Cellular Thermal Shift Assay) technology, this kit provides a convenient no-wash assay for detection and quantitation of small molecule binding to STING, and can be used in hit identification, hit confirmation, and lead optimization studies for increased confidence and better prediction early in the drug discovery process. Please note that a valid CETSA® subscription from Pelago Biosciences is required for use.
Measure binding of small molecule drug candidates to target protein in a cellular environment with Alpha SureFire® CETSA® target engagement assays. For use in combination with Pelago Bioscience's CETSA® (Cellular Thermal Shift Assay) technology, this kit provides a convenient no-wash assay for detection and quantitation of small molecule binding to CDK4, and can be used in hit identification, hit confirmation, and lead optimization studies for increased confidence and better prediction early in the drug discovery process. Please note that a valid CETSA® subscription from Pelago Biosciences is required for use.