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Mar 1, 2009 (Vol. 29, No. 5)

TechNote: High-Throughput Kinase Selectivity Profiling

Bridging the Gulf between Compound Libraries and Rapid Discovery

  • Assay Performance

    Click Image To Enlarge +
    Figure 3. Z’ values were calculated for each kinase based on 16 control wells per experiment in more than 135 independent experiments spanning a period of ten months.

    To assess assay performance of the KINOMEscan platform, we examined the Z´ values for each of the 402 assays. Z´ values were calculated for each kinase based on 16 control wells per experiment in more than 135 independent primary screen experiments spanning a period of 10 months.  The average Z´ value across all of the 402 assays ranges from 0.58 to 0.82 with an average of 0.74 (Figure 3).  Z´ values > 0.5 are indicative of a highly robust assay. 

    To evaluate data consistency, Sunitinib, a multikinase inhibitor, was profiled in 14 independent experiments against the 402-kinase panel over a one-year period at a standard 10 µM concentration.

    Correlation analysis was performed in a pair-wise manner to calculate the correlation coefficients for all possible combinations (Figure 4). The correlation coefficients range from 0.92 to 0.99 with an average of 0.96. Studies using Sorafenib, Erlotinib, and Gefitinib showed similar results (data not shown). These results illustrate the high level of data consistency over time utilizing KINOMEscan.

  • Click Image To Enlarge +
    Figure 4. Profiling of Sunitinib (10 µM) in 14 independent experiments against 402 kinases over one year

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