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scanTK Kinase Assay Panel

scanTK is the largest commercial panel of tyrosine kinases that includes a set of 135 both receptor and non-receptor kinases, plus important mutant forms. scanTK provides a comprehensive understanding of compound binding within the tyrosine kinase family and may serve to opportunistically identify unanticipated interactions leading to expanded therapeutic utility of compounds or as advanced starting points for new programs.

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Panel Features & Benefits

  • The largest panel of receptor and non-receptor tyrosine kinase assays available
  • High-quality reproducible data
  • Rapid turnaround time
  • Dynamic dynamic range: can 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' = 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

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].

scanTK 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(F317I)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317I)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317L)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317L)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(H396P)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(H396P)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(M351T)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Q252H)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Q252H)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(T315I)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(T315I)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Y253F)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL2v-abl Abelson murine leukemia viral oncogene homolog 2 (arg, Abelson-related gene)ABL2
ALKanaplastic lymphoma receptor tyrosine kinaseALK
ALK(C1156Y)anaplastic lymphoma receptor tyrosine kinaseALK
ALK(L1196M)anaplastic lymphoma receptor tyrosine kinaseALK
AXLAXL receptor tyrosine kinaseAXL
BLKB lymphoid tyrosine kinaseBLK
BMXBMX non-receptor tyrosine kinaseBMX
BRKprotein tyrosine kinase 6PTK6
BTKBruton agammaglobulinemia tyrosine kinaseBTK
CSF1Rcolony stimulating factor 1 receptorCSF1R
CSF1R-autoinhibitedcolony stimulating factor 1 receptorCSF1R
CSKc-src tyrosine kinaseCSK
CTKmegakaryocyte-associated tyrosine kinaseMATK
DDR1discoidin domain receptor tyrosine kinase 1DDR1
DDR2discoidin domain receptor tyrosine kinase 2DDR2
EGFRepidermal growth factor receptorEGFR
EGFR(E746-A750del)epidermal growth factor receptorEGFR
EGFR(G719C)epidermal growth factor receptorEGFR
EGFR(G719S)epidermal growth factor receptorEGFR
EGFR(L747-E749del, A750P)epidermal growth factor receptorEGFR
EGFR(L747-S752del, P753S)epidermal growth factor receptorEGFR
EGFR(L747-T751del,Sins)epidermal growth factor receptorEGFR
EGFR(L858R)epidermal growth factor receptorEGFR
EGFR(L858R,T790M)epidermal growth factor receptorEGFR
EGFR(L861Q)epidermal growth factor receptorEGFR
EGFR(S752-I759del)epidermal growth factor receptorEGFR
EGFR(T790M)epidermal growth factor receptorEGFR
EPHA1EPH receptor A1EPHA1
EPHA2EPH receptor A2EPHA2
EPHA3EPH receptor A3EPHA3
EPHA4EPH receptor A4EPHA4
EPHA5EPH receptor A5EPHA5
EPHA6EPH receptor A6EPHA6
EPHA7EPH receptor A7EPHA7
EPHA8EPH receptor A8EPHA8
EPHB1EPH receptor B1EPHB1
EPHB2EPH receptor B2EPHB2
EPHB3EPH receptor B3EPHB3
EPHB4EPH receptor B4EPHB4
EPHB6EPH receptor B6EPHB6
ERBB2erb-b2 receptor tyrosine kinase 2ERBB2
ERBB3erb-b2 receptor tyrosine kinase 3ERBB3
ERBB4erb-b2 receptor tyrosine kinase 4ERBB4
FAKPTK2 protein tyrosine kinase 2PTK2
FERfer (fps/fes related) tyrosine kinaseFER
FESfeline sarcoma oncogeneFES
FGFR1fibroblast growth factor receptor 1FGFR1
FGFR2fibroblast growth factor receptor 2FGFR2
FGFR3fibroblast growth factor receptor 3FGFR3
FGFR3(G697C)fibroblast growth factor receptor 3FGFR3
FGFR4fibroblast growth factor receptor 4FGFR4
FGRFGR proto-oncogene, Src family tyrosine kinaseFGR
FLT1fms-related tyrosine kinase 1 (vascular endothelial growth factor/vascular permeability factor receptor)FLT1
FLT3fms-related tyrosine kinase 3FLT3
FLT3(D835H)fms-related tyrosine kinase 3FLT3
FLT3(D835V)fms-related tyrosine kinase 3FLT3
FLT3(D835Y)fms-related tyrosine kinase 3FLT3
FLT3(ITD)fms-related tyrosine kinase 3FLT3
FLT3(ITD,D835V)fms-related tyrosine kinase 3FLT3
FLT3(ITD,F691L)fms-related tyrosine kinase 3FLT3
FLT3(K663Q)fms-related tyrosine kinase 3FLT3
FLT3(N841I)fms-related tyrosine kinase 3FLT3
FLT3(R834Q)fms-related tyrosine kinase 3FLT3
FLT3-autoinhibitedfms-related tyrosine kinase 3FLT3
FLT4fms-related tyrosine kinase 4FLT4
FRKfyn-related kinaseFRK
FYNFYN oncogene related to SRC, FGR, YESFYN
HCKhemopoietic cell kinaseHCK
IGF1Rinsulin-like growth factor 1 receptorIGF1R
INSRinsulin receptorINSR
INSRRinsulin receptor-related receptorINSRR
ITKIL2-inducible T-cell kinaseITK
JAK1(JH1domain-catalytic)Janus kinase 1JAK1
JAK1(JH2domain-pseudokinase)Janus kinase 1JAK1
JAK2(JH1domain-catalytic)Janus kinase 2JAK2
JAK3(JH1domain-catalytic)Janus kinase 3JAK3
KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(A829P)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(D816H)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(D816V)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(L576P)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D,T670I)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D,V654A)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT-autoinhibitedv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
LCKlymphocyte-specific protein tyrosine kinaseLCK
LTKleukocyte receptor tyrosine kinaseLTK
LYNv-yes-1 Yamaguchi sarcoma viral related oncogene homologLYN
MERTKc-mer proto-oncogene tyrosine kinaseMERTK
METmet proto-oncogene (hepatocyte growth factor receptor)MET
MET(M1250T)met proto-oncogene (hepatocyte growth factor receptor)MET
MET(Y1235D)met proto-oncogene (hepatocyte growth factor receptor)MET
MST1Rmacrophage stimulating 1 receptor (c-met-related tyrosine kinase)MST1R
MUSKmuscle, skeletal, receptor tyrosine kinaseMUSK
PDGFRAplatelet-derived growth factor receptor, alpha polypeptidePDGFRA
PDGFRBplatelet-derived growth factor receptor, beta polypeptidePDGFRB
PYK2PTK2B protein tyrosine kinase 2 betaPTK2B
RETret proto-oncogeneRET
RET(M918T)ret proto-oncogeneRET
RET(V804L)ret proto-oncogeneRET
RET(V804M)ret proto-oncogeneRET
ROS1c-ros oncogene 1 , receptor tyrosine kinaseROS1
SRCSRC proto-oncogene, non-receptor tyrosine kinaseSRC
SRMSsrc-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sitesSRMS
SYKspleen tyrosine kinaseSYK
TECtec protein tyrosine kinaseTEC
TIE1tyrosine kinase with immunoglobulin-like and EGF-like domains 1TIE1
TIE2TEK tyrosine kinase, endothelialTEK
TNK1tyrosine kinase, non-receptor, 1TNK1
TNK2tyrosine kinase, non-receptor, 2TNK2
TRKAneurotrophic tyrosine kinase, receptor, type 1NTRK1
TRKBneurotrophic tyrosine kinase, receptor, type 2NTRK2
TRKCneurotrophic tyrosine kinase, receptor, type 3NTRK3
TXKTXK tyrosine kinaseTXK
TYK2(JH1domain-catalytic)tyrosine kinase 2TYK2
TYK2(JH2domain-pseudokinase)tyrosine kinase 2TYK2
TYRO3TYRO3 protein tyrosine kinaseTYRO3
VEGFR2kinase insert domain receptor (a type III receptor tyrosine kinase)KDR
YESv-yes-1 Yamaguchi sarcoma viral oncogene homolog 1YES1
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