scanELECT Kinase Selectivity & Profiling Assay Panel

A flexible approach to personalized screening

A flexible 'a la carte' approach for customized kinase profiling.  Select from KINOMEscan's collection of 451 kinase assays and build your own customized assay panel of any size comprising only of kinases relevant to your programs.  A simple, fast and cost-effective alternative to in-house assay development and screening.  Ideal for any size compound collection (low to high throughput), and data turnaround within  five business days is available for ongoing scheduled projects.  scanELECT is an extremely flexible solution wth multiple applications including, primary HTS & lead discovery and ongoing lead optimization & SAR.


 

Panel Highlights and Benefits

  • Customized selectivity profiling - select from over 
    450 kinase assays
  • High-quality reproducible data
  • Rapid turnaround time (5 - 10 business days)
  • Broad dynamic range: can 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
scanMAX Kinase Dendrogram


Red circles (above) represent the kinases currently available in the KINOMEscan panel.  Individual assays can be selected and rapidly screened using scanELECT.

Assay Sensitivity

Assay Sensitivity and Range
Binding constant (Kd) determinations for the indicated compounds against LOK demonstrate the broad range of interaction affinities quantitatively measured using the KINOMEscan assay platform [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' = 0.72 [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

Imatinib and ABL1 type II compound

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].