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Benefits - KINOMEscan®

KINOMEscan is the leading provider of selectivity profiling services for kinase inhibitor drug discovery. Leveraging our panel of over 450 kinase assays and our kinase inhibitor drug discovery expertise, KINOMEscan provides investigators the benefit of kinome-wide profiling, the flexibility to create personalized screening solutions, and the knowledge to support and inform decision making throughout the kinase drug development continuum.

As experts in kinase focused drug discovery, our knowledge base encompasses many disciplines, including kinase inhibitor drug discovery, kinase biology & biochemistry, and laboratory automation and screening operations. We pride ourselves on a proven track record of successful partnerships with organizations of all sizes and helping our partners to extract the maximum value from their kinase-focused chemical assets.

Key Benefits

  • Largest commercial kinase assay panel available - 456 total assays
  • Flexible – low to high throughput and predefined or personalized kinase assay panel selection
  • Rapid data turnaround
  • Accurate, precise & reproducible data
  • ATP not required: delivers true thermodynamic affinity data as opposed to IC50s
  • Detection of multiple inhibitor types, including type I, type II, and allosteric
  • Includes activation state-specific assays that provide inhibitor binding mode information
  • Large dynamic range for accurate affinity measurement

World's Largest Kinase Panel - 456 Kinase Assays

Covers greater than 80% of the ‘typical’ human protein kinome and includes a definitive set of 456 kinases covering AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid and atypical kinase families, pathogen kinases, and important disease relevant mutant forms. Also includes activation state-specific assays to provide inhibitor binding mode information. 

  • More than 80% of the human protein kinome
  • 453 human kinase assays plus 3 pathogen kinases
  • 132 tyrosine kinase assays
  • 56 disease-relevant mutants
  • 20 lipid kinase assays
  • Activation state-specific assays

scanMAX Kinase Dendrogram
 
Red circles (above) represent the kinases currently available in the KINOMEscan panel.

Flexible Screening Solutions

KINOMEscan provides ready access to a portfolio of more than 450 high-quality kinase assays, a suite of integrated solutions, user-defined screening parameters and flexible service models to support your discovery goals and to maximize program success rates.

  • Preselected assay panels - choose any of our defined assay panels or create your own
  • Personalized assay panels - build a customized panel by selecting only your assays of interest
  • Screening concentration - used-defined screening concentrations 
  • Throughput - easily accommodate 1-1000's of compounds against our entire kinase panel or a subset
  • Follow up studies - binding affinity determinations, compound reversibility & more
  • Multiple business models - fee for service, subscription & prepaid screening models available

Rapid data turnaround

Rapid, reliable data turnaround is essential for keeping programs on track, on time and on budget. Standard data turnaround for study requests is 10 business days from compound receipt, with 5 business day turnaround available for regularly scheduled ongoing screening programs and subscription services. Average data turnaround is eight business days.

Data Turnaround

Study Report Data turnaround
Average data turnaround for 2009 - 2010 calendar years was 8.0 days. Ninety percent of study reports were delivered within ten business days of compound receipt at KINOMEscan. Large projects such as compound library profiling, and single target high-throughput screening may vary depending on scale.

 



















Accurate, precise & reproducible data

KINOMEscan screening partners have long recognized that accurate, precise and reproducible kinase profiling data are critical components of the discovery and development process and are the cornerstone of a successful screening partnership. All KINOMEscan assays undergo thorough validation prior to being released into production and assay performance is continually monitored to ensure data consistency & longitudinal concordance.

  • Data accuracy and precision have been demonstrated in several peer-reviewed publications from both the KINOMEscan team and our partners.

Assay quality: Primary screen reproducibility

  • Outstanding screen to screen reproducibility
  • Enables data to be interpreted with confidence

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].























Assay quality: Z’ values

  • 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 rates

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' = 0.71 [click graph to enlarge].






















Detect multiple types of kinase inhibitors

Although the majority of kinase inhibitors developed so far have been type I or type II inhibitors that fully or partially overlap the ATP binding site, there are also examples of non-ATP competitive “allosteric” inhibitors that target the kinase active site and inhibit catalysis by repositioning key catalytic residues. Allosteric inhibition may represent a promising strategy for the development of highly potent & selective compounds. KINOMEscan affords investigators a flexible screening solution for detecting these multiple inhibitor types and to thereby extract the maximum value from their chemical assets.


Detection of Type I, II & Allosteric Inhibitors

Binding constant (Kd) determinations were measured for interactions between gefitinib, a known Type I inhibitor and EGFR (Kd = 3.4nM); imatinib, a known Type II inhibitor and KIT (Kd = 7.5nM); and CI-104, a known non-ATP-competitive inhibitor and MEK1 (Kd = 120nM). These data illustrate the diversity of inhibitor types detected in KINOMEscan assays [click graph to enlarge].























Large dynamic range for accurate affinity measurements

KINOMEscan binding assays use low kinase concentrations (less than 0.1 nM). This feature, coupled with quantitative, precise and ultra-sensitive qPCR readout, affords a large dynamic range (greater than five logs) for the measurement of accurate affinity values (Kd less than 100 pM to greater than 10 uM). These features provide a flexible, sensitive and highly quantitative platform for the identification and discrimination of a wide spectrum of inhibitors.

Assay Sensitivity

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].