As a result, conventional target engagement assays increase the risk that you will prioritize ineffective compounds, at great cost to your company as well as to your own goals. This measures target engagement within the natural environment of living intact cells, lysates, and even tissues, without modifying the compounds or target proteins. Invented in , CETSA leverages the basic principle of thermal shift assays, with the novel insight that the melt curves of proteins can be measured in living cells.
Compared to conventional biophysical approaches, this label-free measure of affinity offers a more accurate, direct measurement of drug-target binding in a more physiologically relevant manner. As such, CETSA gives you true target engagement potencies, enabling you to make more reliable predictions of efficacy. CETSA is also available in three formats.
Platform differentiated by foundational scientific advances:
These provide additional flexibility, as they allow the assay to be applied at any stage of drug discovery, including in early lead generation as well as in later lead optimization. The three formats are:. By enabling you to make confident prioritization decisions at a discovery stage as early as lead generation, CETSA helps you avoid the risk of investing in the wrong compounds and ensures you progress only the very best compounds through the pipeline. Leading pharmaceutical and biotech companies are already prospering from the many benefits CETSA can bring to lead generation and lead optimization studies.
Embracing change by adopting such novel methods can provide you with high-quality, relevant data for making better-informed prioritization decisions, so that you invest in only the best compounds. Not only will this allow you to accelerate ahead of your competitors, but by progressing only the very best compounds, you will also be helping to reduce attrition in drug discovery and bring essential new treatments to patients. Are you using the right target engagement assays for your drug discovery program?
Measuring target engagement for drug discovery: A change for the better In drug discovery programs, target engagement assays are vital tools for identifying which compounds to prioritize for further investment. How can a novel target engagement assay revolutionize your research? This uses a Western blot detection method and is valuable for screening a handful of compounds in low-throughput and translational studies.
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Theme: Innovation for the Next Generation of Therapeutics
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