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Scientific publication

Mechanism of Action for Degraders

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...
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Compound Evaluation and Potency Ranking

It is a well-established fact in basic science, as well as in drug discovery, that the differences between an assay based on a purified or recombinant protein and a full-length protein in a native cellular context may have substantial impact on the data. This will...
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Target Deconvolution

Since the protein targets of any given compound hit from a phenotypic screen are initially unknown, one major challenge with phenotypic-based drug discovery is the need for target identification or deconvolution. Choosing the most efficient and reliable method for...
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Hit Confirmation

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. CETSA® requires no protein or ligand modifications...
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Target Engagement

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...
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Biomarker Discovery

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...
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CETSA® on Membrane Proteins

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...
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Preclinical Development

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...
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Lead Optimization

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...
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Selectivity

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...
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Target Validation

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...
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Library Screening

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...
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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...
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Translational studies

CETSA® can assess target engagement across a multitude of sample types. Established assays can easily be transferred from cell line to animal tissue, human primary cells, or patient-derived material, and thereby be used for translation all the way from lab bench...

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