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.