scanEDGE Kinase Assay Panel

96 assays - an economical approach to surveying the human kinome

An economical approach to surveying the human kinome, scanEDGE includes 96 kinases distributed throughout the AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid, and atypical kinase families, plus important mutant forms. scanEDGE is an economical alternative to scanMAX and useful to assess compound selectivity at all stages of drug discovery and development, from lead discovery & hit identification to lead optimization.  Assays may be substituted to create a custom solution for your specific program requirements, and with five business day turnaround available, scanEDGE is an ideal solution for SAR and lead optimization activity.

Panel Highlights and Benefits

  • Panel of 96 kinases distributed across the kinome
  • High-quality reproducible data
  • Rapid turnaround time
  • Broad dynamic range: detect compounds with Kds <100 pM to >10 mM
  • Flexible - standard and custom panels
  • Detection of multiple inhibitor types (e.g. type I, II & non-ATP competitive) 
  • Economically priced
scanEDGE Kinase Dendrogram

Red circles (above) represent all kinases currently available in the KINOMEscan panel. Blue circles represent assays included in the scanEDGE panel.

Assay Sensitivity

Assay Sensitivity and Range

Binding constant (Kd) determinations for the indicated compounds against LOK demonstrate the broad range (> 5 logs) of interaction affinities quantitatively measured using the KINOMEscan assay platform.  Assays are performed at low kinase concentrations (<0.1 nM), which enables the measurement of accurate Kd values in the pM range [click graph to enlarge].

Assay Quality

Z' Factor Analysis - one metric of assessing assay quality

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' for all assay is 0.71 [click graph to enlarge].

 

Data Consistency


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].

Detection of Type II Kinase Inhibitors

Activation State Specific Kinase Inhibitor Imatinib and phosphorylated ABL1

Binding constant (Kd) determinations were measured for interactions between imatinib, a known Type II inhibitor, and ABL preparations differentially phosphorylated on the A-loop.  Imatinib exhibited a 30-fold affinity preference for the non-phosphorylated state (Kd = 1.4 nM) relative to the phosphorylated state (Kd = 56 nM) [click graph to enlarge].