When would you like to know if your Compound really is Therapeutic?
Early discovery or late confirmation? Proteomic-wide profiling or a few carefully selected targets? Both approaches are important tools in drug discovery. But it turns out that the choice between a broad and narrow scope is often driven by non-scientific factors like ideology, habit and upfront costs.
Better tools are needed to push the boundaries in drug discovery and uncover new medicines. However, despite increasing investment in research and development, the majority of candidates still fail in clinical trials. It’s thought that over half of these failures are due to a lack of efficacy in proof-of-concept trials – a subject of much debate in the industry.
Finding ways to minimize late-stage failures is more vital than ever before. We therefore need to be able to better predict which compounds will fail much earlier in the drug discovery pipeline so that only the very best ones are prioritized from the outset.
For a drug to be effective and safe, the compound must selectively bind to the target protein at the intended site of action, a process known as target engagement (TE). As such, measurements are already routinely used for selecting CDs with sufficient TE, but the high rate of efficacy failures during clinical trials shows that these conventional approaches are not working.
The Cellular Thermal Shift Assay (CETSA®) enables direct, physiologically relevant TE quantification within intact cells and tissues, based on the fundamental principle of thermal shift assays