scanMAX Kinase Assay Panel

451 Assays - the most comprehensive kinase assay panel

The largest commercial kinase panel available, scanMAX contains a set of 451 kinases covering AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid and atypical kinase families, plus important mutant forms. scanMAX is an ideal choice for all stages of drug discovery and development,  from lead discovery & hit identification to lead optimization, preclinical and compound safety. 

Kinome-wide annotation of compound selectivity enables informed decisions about therapeutic opportunities and potential off-target liabilities which could otherwise be missed in smaller kinase panels. Panel includes: 448 human kinases, 3 pathogen kinases, 54 disease relevant mutants, 130 tyrosine kinase assays, and 20 lipid kinases.
 

Panel Highlights and Benefits

  • More than 80% coverage of the human protein kinome
  • High-quality reproducible data
  • Rapid turnaround time
  • Broad dynamic range: can detect compounds with Kds <100 pM to >10 mM
  • Flexible - Standard and custom panels
  • Activation-state specific assays
  • Detection of multiple inhibitor types (e.g. type I, II & non-ATP competitive)
scanMAX Kinase Dendrogram

Red circles represent the kinases currently available in the KINOMEscan panel.

Assay Sensitivity, Quality, Reproducibility & Type II Interactions

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].