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How does cellular target engagement relate to efficacy?

The patented Cellular Thermal Shift Assay (CETSA®) helps you to circumvent this persistent problem. CETSA® EC50 determines the potency of compounds directly in the cells or tissues of interest, providing crucial information about target engagement independent from function, early in the drug discovery pipeline.

CETSA® EC50 correlates with other measures of affinity.

  • CETSA® EC50 provides you with the relative potency of your compound, allowing you to rank and prioritise lead compounds in the native physiological environment.
  • CETSA® can accelerate your drug discovery pipeline by evaluating your compound’s target engagement in relevant tissues – before risks and costs escalate.
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How does cellular target engagement relate to efficacy? Download our CETSA® Navigate application note.

Publications

  1. Martinez Molina et al. Science 2013

  2. Jafari et al.Nature Protocols 2014

  3. Ishii et al. Nature Scientific Reports 2017

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