Rank compound
potency in cells,
not just in vitro
Potency ranking addresses the gap between biochemical activity and cellular relevance by quantifying target engagement directly in cells. Concentration–response data and EC₅₀ estimates generated in native biological systems provide a more reliable basis for prioritizing compounds and chemical series, thereby helping to focus SAR efforts on areas with the greatest potential impact.
Standardized concentration–response experiments are used to rank compounds across chemotypes, with careful attention to assay format, experimental conditions, and model relevance. Decisions around concentration range, replication, and data normalization are made to ensure that potency estimates are robust and comparable across assay runs and experimental campaigns. Curve quality, fit parameters, and acceptance criteria are defined in advance to support consistent interpretation.
Throughout this phase, assay performance and data quality are monitored to generate decision-ready potency rankings. These data guide chemistry design cycles, support the deprioritization of lower-value series, and establish a solid foundation for downstream lead optimization by ensuring that comparisons across series are based on reliable and biologically meaningful measurements.
Rank by real engagement: Targeted Profiling
CETSA-based measurements ensure that cellular potency reflects meaningful target engagement rather than assay-specific effects. This adds biological context to EC₅₀ estimates and helps prioritize series based on engagement-driven activity rather than apparent biochemical strength alone.
Potency ranking is enabled by our Targeted Profiling Service
Targeted Profiling
Validate mechanistic hypotheses and confirm that on-target engagement occurs in the intended cellular context.
No target – no therapy
Discover how potency ranking with CETSA helps you rank and prioritize drug candidates early in the discovery process.
Are you using the right tools?
Early integration of CETSA technology can help you streamline your discovery pipeline, minimize late-stage failures, and uncover novel targets faster than traditional methods.
What is CETSA?
Why work directly in cells?
Our webinars
Drug discovery insights with CETSA
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A mass spectrometry approach for target ID and compound profiling
In this webinar, you will find a presentation of various applications of CETSA® Explore, highli…
Is Your Hit on Target?
Validate Early with CETSA® Accelerate hit confirmation and lead optimization with CETSA® …
No Target, No Therapy – Target Engagement with CETSA®
Direct Insights into Target Engagement with CETSA® Discover how potency ranking with CETSA help…