Potency ranking is essential in the lead optimization phase of drug discovery for selecting and refining compounds with strong target engagement.
CETSA measures how well a compound binds to its target in intact, biologically relevant cells, ensuring relevance to disease models. This helps establish a clear link between cellular target engagement and functional readouts, helping to establish a clear Structure-Activity Relationship (SAR) and ensuring that potency improvements translate into biological effects.
Integrating CETSA into your assay cascade and using CETSA derived potency values to guide compound design will help you to make more informed design decisions and prioritize compounds with the highest potential for success. This approach significantly reduces the risk of costly late-stage failures by further ensuring only compounds with relevant target engagement progress.
Key Benefits
- Biologically Relevant Potency Data – Measure target engagement in intact cells, ensuring potency rankings reflect real-world disease models.
- Stronger SAR Development – Establish a clear relationship between compound binding and functional biological effects.
- Reduced Late-Stage Attrition – Prioritize compounds with verified cellular target engagement to lower the risk of failures in later development stages.
How it works
- Assay Design and Validation—We develop customized assays to ensure robust, reproducible results specific to your target and compounds.
- Potency Ranking – Concentration-response measurement of compound binding within a native cellular environment generating CETSA-derived EC50 values.
- Data Analysis and Prioritization – In-depth evaluation of target engagement data to enable and guide compound design and identify the most promising candidates for further development.