Biomarkers are important to facilitate translation, validate the therapeutic hypothesis and monitor therapeutic effect in clinical trials and beyond. The identification of biomarkers is a time-demanding but crucial part of the preclinical drug discovery…
CETSA® has primarily been applied to soluble proteins which, upon heating, denaturate to form insoluble aggregates by exposing hydrophobic surfaces. Nevertheless, CETSA® has successfully been applied to a number of membrane-associated proteins including…
In late-stage lead optimization, before CD selection, a smaller set of compounds are further investigated. The aim here is to ensure that the CD (or CDs) ultimately selected is safe for clinical testing as well as suitable for formulation and that other pre-clinical drug…
The aim at this stage of the drug discovery and development process is to optimize the compound properties to ensure the development of safe and effective candidate drugs (CDs) that can be dosed in healthy volunteers. Structure-activity relationship (SAR) analysis is used for guidance…
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…
Reliable data probing the disease-related hypothesis for a potential therapeutic target is crucial throughout the drug discovery and development process. The ultimate target validation is not achieved until the proof-of-concept study in phase 2 patient…
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…
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…
As CETSA® can be performed in live cells or tissue, the CETSA® EC50 values give you a consistent reference point that can enable translation as your compounds move from lead generation into lead…