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KINOMEscan® Assay Platform

The KINOMEscan screening platform employs a novel and proprietary active site-directed competition binding assay to quantitatively measure interactions between test compounds and more than 450  kinase assays and disease relevant mutant variants. This robust and reliable assay technology affords investigators the ability to annotate compounds with accurate, precise and reproducible data. KINOMEscan assays do not require ATP and thereby report true thermodynamic interaction affinities, as opposed to IC50 values, which can depend on the ATP concentration.

Overview & Assay Principle

Compounds that bind the kinase active site and directly (sterically) or indirectly (allosterically) prevent kinase binding to the immobilized ligand, will reduce the amount of kinase captured on the solid support (Panels A & B). Conversely, test molecules that do not bind the kinase have no effect on the amount of kinase captured on the solid support (Panel C). Screening “hits” are identified by measuring the amount of kinase captured in test versus control samples by using a quantitative, precise and ultra-sensitive qPCR method that detects the associated DNA label (Panel D). In a similar manner, dissociation constants (Kds) for test compound-kinase interactions are calculated by measuring the amount of kinase captured on the solid support as a function of the test compound concentration.  Learn more about the assay process > 
 

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Performance Metrics & Data Quality

  • Z’ values measure assay noise and predictive value
  • High Z’ values reproducibly measured across entire assay panel
  • High Z’ values ensure low false positive/negative rate

Assay Quality

   

Primary Screen Reproducibility & Data Consistency

             
Average Z' values and standard deviations were calculated for each kinase based on fourteen control wells per experiment in over 135 independent experiments spanning a period of sixteen months. Average Z' = 0.71 [click graph to enlarge].
   
Profiling of the indicated compounds at 10uM in fourteen independent experiments against 442 kinases over a one year period. Correlation analysis was performed in a pair-wise comparison to calculate the correlation coefficient. The correlation coefficients range from 0.91 to 0.97 with an average of 0.95 [click graph to enlarge].

Assay Platform Features & Benefits

  • Largest commercial kinase assay panel available
  • Flexible – low to high throughput and predefined or personalized assay panel selection
  • ATP not required: delivers true thermodynamic affinity data as opposed to IC50s
  • Detection of multiple inhibitor types, including type I, type II, and allosteric
  • Large dynamic range for accurate affinity measurement

Learn about more KINOMEscan Benefits >