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A majority of drug candidates fail in clinical trials. Many of them fail in late proof-of-concept studies due to a lack of efficacy, which results in increased costs and lost time. This waste of time and resources can be avoided by applying target engagement studies with high accuracy and predictive value early and continuously in the drug discovery value chain. Select a topic to begin.
Including CETSA® in your assay cascade and using the EC50 data for potency ranking within your chemical series facilitates a relevant compound design yielding compounds with higher chance of therapeutic effect.
In drug discovery, selective binding of the compound to the right target is important for the drug to be both effective and safe. To achieve this, the drug must be present at the site of action and occupy the intended target with high specificity.
Targeted protein degradation is a novel modality with the potential to tackle therapeutically interesting proteins beyond the limitations of current existing approaches. In this area, CETSA® is a powerful technology which can be applied for investigating the degradation target
For a drug to be effective according to the target hypothesis, it must selectively bind to the intended target protein to elicit its effect. Target engagement (TE) is defined as the interaction of ligands with their molecular targets. Assessment of a compound’s TE is essential in the discovery and development of new therapies.
CETSA® can determine cellular target engagement in physiologically relevant settings of the native, full-length protein and can potentially unlock novel chemical space. CETSA® library screening in intact cells gives direct confirmation on target engagement of your library compounds in physiological conditions from the onset.
As a cellular target engagement assay that determines the level of interaction between a ligand and a target protein of interest in a physiologically relevant setting, CETSA® is perfectly suited for hit confirmation.