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scanEDGE Kinase Assay Panel

An economical approach to surveying the human kinome, scanEDGE includes 97 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.
 
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Panel Features & Benefits

  • Panel of 97 kinases distributed across the kinome
  • High-quality reproducible data
  • Rapid turnaround time
  • Broad dynamic range: detect compounds with Kds <100 pm to >10 uM
  • Flexible - standard and custom panels
  • Detection of multiple inhibitor types (e.g. type I, II & non-ATP competitive) 
  • Economically priced
How it Works

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].

scanEDGE Assay Panel

Listed below are the assays currently available for screening and profiling.
 
 
KGS ▲Kinase NameEntrez Gene Symbol
ABL1(E255K)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(T315I)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ACVR1Bactivin A receptor, type IBACVR1B
ADCK3coenzyme Q8ACABC1
AKT1v-akt murine thymoma viral oncogene homolog 1AKT1
AKT2v-akt murine thymoma viral oncogene homolog 2AKT2
ALKanaplastic lymphoma receptor tyrosine kinaseALK
AURKAaurora kinase AAURKA
AURKBaurora kinase BAURKB
AXLAXL receptor tyrosine kinaseAXL
BMPR2bone morphogenetic protein receptor, type II (serine/threonine kinase)BMPR2
BRAFv-raf murine sarcoma viral oncogene homolog B1BRAF
BRAF(V600E)v-raf murine sarcoma viral oncogene homolog B1BRAF
BTKBruton agammaglobulinemia tyrosine kinaseBTK
CDK11cyclin-dependent kinase 19CDK19
CDK2cyclin-dependent kinase 2CDK2
CDK3cyclin-dependent kinase 3CDK3
CDK7cyclin-dependent kinase 7CDK7
CDK9cyclin-dependent kinase 9CDK9
CHEK1checkpoint kinase 1CHEK1
CSF1Rcolony stimulating factor 1 receptorCSF1R
CSNK1Dcasein kinase 1, deltaCSNK1D
CSNK1G2casein kinase 1, gamma 2CSNK1G2
DCAMKL1doublecortin-like kinase 1DCLK1
DYRK1Bdual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1BDYRK1B
EGFRepidermal growth factor receptorEGFR
EGFR(L858R)epidermal growth factor receptorEGFR
EPHA2EPH receptor A2EPHA2
ERBB2erb-b2 receptor tyrosine kinase 2ERBB2
ERBB4erb-b2 receptor tyrosine kinase 4ERBB4
ERK1mitogen-activated protein kinase 3MAPK3
FAKPTK2 protein tyrosine kinase 2PTK2
FGFR2fibroblast growth factor receptor 2FGFR2
FGFR3fibroblast growth factor receptor 3FGFR3
FLT3fms-related tyrosine kinase 3FLT3
GSK3Bglycogen synthase kinase 3 betaGSK3B
IGF1Rinsulin-like growth factor 1 receptorIGF1R
IKK-alphaconserved helix-loop-helix ubiquitous kinaseCHUK
IKK-betainhibitor of kappa light polypeptide gene enhancer in B-cells, kinase betaIKBKB
INSRinsulin receptorINSR
JAK2(JH1domain-catalytic)Janus kinase 2JAK2
JAK3(JH1domain-catalytic)Janus kinase 3JAK3
JNK1mitogen-activated protein kinase 8MAPK8
JNK2mitogen-activated protein kinase 9MAPK9
JNK3mitogen-activated protein kinase 10MAPK10
KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(D816V)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D,T670I)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
LKB1serine/threonine kinase 11STK11
MAP3K4mitogen-activated protein kinase kinase kinase 4MAP3K4
MAPKAPK2mitogen-activated protein kinase-activated protein kinase 2MAPKAPK2
MARK3MAP/microtubule affinity-regulating kinase 3MARK3
MEK1mitogen-activated protein kinase kinase 1MAP2K1
MEK2mitogen-activated protein kinase kinase 2MAP2K2
METmet proto-oncogene (hepatocyte growth factor receptor)MET
MKNK1MAP kinase interacting serine/threonine kinase 1MKNK1
MKNK2MAP kinase interacting serine/threonine kinase 2MKNK2
MLK1mitogen-activated protein kinase kinase kinase 9MAP3K9
p38-alphamitogen-activated protein kinase 14MAPK14
p38-betamitogen-activated protein kinase 11MAPK11
PAK1p21 protein (Cdc42/Rac)-activated kinase 1PAK1
PAK2p21 protein (Cdc42/Rac)-activated kinase 2PAK2
PAK4p21 protein (Cdc42/Rac)-activated kinase 4PAK4
PCTK1cyclin-dependent kinase 16CDK16
PDGFRAplatelet-derived growth factor receptor, alpha polypeptidePDGFRA
PDGFRBplatelet-derived growth factor receptor, beta polypeptidePDGFRB
PDPK13-phosphoinositide dependent protein kinase-1PDPK1
PIK3C2Bphosphoinositide-3-kinase, class 2, beta polypeptidePIK3C2B
PIK3CAphosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CGphosphoinositide-3-kinase, catalytic, gamma polypeptidePIK3CG
PIM1pim-1 oncogenePIM1
PIM2pim-2 oncogenePIM2
PIM3pim-3 oncogenePIM3
PKAC-alphaprotein kinase, cAMP-dependent, catalytic, alphaPRKACA
PLK1polo-like kinase 1PLK1
PLK3polo-like kinase 3PLK3
PLK4polo-like kinase 4PLK4
PRKCEprotein kinase C, epsilonPRKCE
RAF1v-raf-1 murine leukemia viral oncogene homolog 1RAF1
RETret proto-oncogeneRET
RIOK2RIO kinase 2RIOK2
ROCK2Rho-associated, coiled-coil containing protein kinase 2ROCK2
RSK2(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 3RPS6KA3
SNARKNUAK family, SNF1-like kinase, 2NUAK2
SRCSRC proto-oncogene, non-receptor tyrosine kinaseSRC
SRPK3SFRS protein kinase 3SRPK3
TGFBR1transforming growth factor, beta receptor 1TGFBR1
TIE2TEK tyrosine kinase, endothelialTEK
TRKAneurotrophic tyrosine kinase, receptor, type 1NTRK1
TSSK1Btestis-specific serine kinase 1BTSSK1B
TYK2(JH1domain-catalytic)tyrosine kinase 2TYK2
ULK2unc-51-like kinase 2ULK2
VEGFR2kinase insert domain receptor (a type III receptor tyrosine kinase)KDR
YANK3serine/threonine kinase 32CSTK32C
ZAP70zeta-chain (TCR) associated protein kinase 70kDaZAP70
 

Data Analysis & Interpretation

Definitions

Percent of Control (%Ctrl)

The results for single concentration (primary screen) binding interactions for tested compound(s) are reported in your study report and spreadsheets as '%Ctrl' and is calculated in the following manner:

    test compound = client supplied compound
    negative control = DMSO (100% control)
    positive control = control compound (0% control)

Binding Constant (Kd)

The results for an 11-point dose response curve compound/kinase interactions are reported in your study report and spreadsheets as Kd, which are values derived using the Hill equation:
Hill equation used for calculating binding constants
The Hill Slope is set to -1. Curves are fitted using a non-linear least square fit with the Levenberg-Marquardt algorithm.

Selectivity Score (S-Scores)

Selectivity Score or S-score is a quantitative measure of compound selectivity. It is calculated by dividing the number of kinases that compounds bind to by the total number of distinct kinases tested, excluding mutant variants.
selectivity score calculation

This value can be calculated using %Ctrl as a potency threshold (below) and provides a quantitative method of describing compound selectivity to facilitate comparison of different compounds.

   S(35) = (number of non-mutant kinases with %Ctrl <35)/(number of non-mutant kinases tested)

   S(10) = (number of non-mutant kinases with %Ctrl <10)/(number of non-mutant kinases tested)

     S(1) = (number of non-mutant kinases with %Ctrl <1)/(number of non-mutant kinases tested)

Using S-Score Data to Quantitate Selectivity

Selectivity Profile for 38 Small Molecule Kinase Inhibitors

32 small molecule compound calibration curve
KINOMEscan's in vitro competition binding assay was used to evaluate 38 kinase inhibitors against a panel of 287 distinct human protein kinases (~55% of the predicted human protein kinome), and three lipid kinases. The compounds tested included 21 tyrosine kinase inhibitors, 15 serine-threonine kinase inhibitors, 1 lipid kinase inhibitor, and staurosporine. S(35), 10uM = (number of non-mutant kinases with %Ctrl <35)/(290 kinases tested; 27 mutant variants were excluded from this analysis). Compounds approved for use in humans (as of August, 2007) are highlighted (gray bars)  [click graph to enlarge].

TREEspot Kinase Dendrograms: A Visual Representation of Compound Selectivity

TREEspot is an innovative compound profile visualization tool for visualizing screening data. Kinases found to bind are marked with red circles, where larger circles indicate higher-affinity binding.

RSK Inhibitor 

RSK Inhibitor small panel versus large panel selectivity

RSK inhibitor was reported in published findings to be a selective RSK kinase inhibitor on the basis of kinase profiling against a panel of 54 kinases.  Selectivity profiling against the scanMAX kinase assay panel (then 402) revealed additional interactions not previously identified [click graph to enlarge].

TREEspot Compound Profile Visualization Tool

TREEspot is an innovative, secure access, web-based, compound profile visualization tool for analysis of KINOMEscan screening data. TREEspot is an ideal companion tool for existing data analysis applications and facilitates compound profile visualization through its simple yet powerful user interface.

Gain new perspectives of kinase profile data in a visual environment and distill essential knowledge to drive your discovery programs.  TREEspot is provided as a complimentary tool to our clients. To learn more about how you can visualize your data using TREEspot or to request access credentials, please contact KINOMEscan.

  • Easy-to-use
  • Facilitates evaluation and analysis of profiling data
  • Generates publication quality of TREEspot images
  • Provides global visualization of profile data
  • Visualize your data in a whole new way
 

scanMAX Kinase Dendrogram