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tkMAXSM - Tyrosine Kinase Assay Panel

tkMAX is a growing panel of 25 functional, cell-based tyrosine kinase (TK) assays ideal for identifying novel inhibitors, characterizing compounds and confirming hits from a biochemical screen. Unlike biochemical assays that commonly use a truncated version of the receptor, tkMAX utilizes the wild type, full length proteins which allow all steps in receptor activation to be monitored. This whole cell assay platform is ideal for identifying novel tyrosine kinase inhibitors, allosteric modulators or antibody therapeutics. 

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Panel Features & Benefits

  • Comprehensive panel of 25 validated cell based kinase assays
  • Standardized assay conditions for reliable comparison across all receptor types
  • Run in inhibitor mode – identify small molecule inhibitors and/or antibody therapeutics
  • Regularly scheduled panel dates 
  • Broad applications – including target identification, specificity and selectivity
  • Use in combination with KINOMEscan platform to confirm biochemical screening hits
How it Works

Receptor Tyrosine Kinases - Ideal for Small Molecule and Antibody Discovery

Unlike biochemical assays that commonly use a truncated version of the receptor, our cell-based kinase assay utilize wild-type, full length proteins that allow all steps in receptor activation to be monitored.  This whole cell assay platform is ideal for identifying novel receptor tyrosine kinase inhibitors, allosteric modulators or antibody therapeutics.
 
A series of commercially available anti-receptor antibodies (neutralizing antibodies) were tested with cells expressing the ErbB1 receptor and dose dependent inhibition was observed (left panel).  Cells expressing TrkA, TrkB, or TrkC were used to identify, screen or profile small molecule inhibitors (right panel).

tkMAX Assay Panel

Listed below are the assays currently available for screening and profiling.
 
 
Gene Symbol ▲Kinase NameEntrez Gene Symbol
c-KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT)c-KIT
c-Ret-GFRα2Proto-oncogene tyrosine-protein kinase receptor Ret (RET)c-Ret-GFRα2
DDR1Discoidin domain receptor 1 (CD167a)DDR1
EphA5Ephrin type-A receptor 5 (EphA5)EphA5
EphA7Ephrin type-A receptor 7 (EphA7)EphA7
EphB2Ephrin type-B receptor 2 (EphB2)EphB2
EphB3Ephrin type-B receptor 3 (EphB3)EphB3
EphB4Ephrin type-B receptor 4 (EphB4)EphB4
ErbB1v-erb-b2 erythroblastic leukemia viral oncogene homolog 1 (EGFR)ErbB1
ErbB2-ErbB3v-erb-b2 erythroblastic leukemia viral oncogene homolog 2 (HER2)ErbB2-ErbB3
ErbB4erb-b2 receptor tyrosine kinase 4ErbB4
FGRFGR proto-oncogene, Src family tyrosine kinase (FGR)FGR
FLT4fms-related tyrosine kinase 4 (FLT4)FLT4
IGF1RInsulin-like growth factor 1 receptor (IGF1R)IGF1R
INSRbInsulin receptor, isoform B (INSR)INSRb
JAK3Janus kinase 3 (JAK3)JAK3
KDRKinase Insert Domain Receptor (VEGFR2)KDR
PDGFRaPlatelet-derived growth factor receptor alpha (PDGFRa)PDGFRa
PDGFRbPlatelet-derived growth factor receptor beta (PDGFRb)PDGFRB
PRLR-JAK1Prolactin receptor (PRLR)PRLR-JAK1
PRLR-JAK2Prolactin receptor (PRLR)PRLR-JAK2
TrkA-P75Neurotrophic tyrosine kinase receptor type 1 (NTRK1)TrkA-P75
TrkB-P75Neurotrophic tyrosine kinase receptor type 2 (NTRK2)TrkB-P75
TrkC-P75Neurotrophic tyrosine kinase receptor type 3 (NTRK3)TrkC-P75
TYK2Tyrosine kinase 2 (TYK2)TYK2

Data Analysis & Interpretation 

Definitions

Percent Activity/Inhibition

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

% Activity
(Agonist Mode) =
100% x
[
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

 

% Inhibition
(Antagonist mode) =
100% x
[ 1- 
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity) 

 

Dose Response Curve (EC50/IC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:

hill equation

To ensure your compounds are included in the Test Date of your choosing, submit your compounds and PO by the date indicated in the "Compounds & PO Due" column below.

2017 gpcrMAX and orphanMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing
gpcrMAX,
orphanMAX
January 31 January 27 February 28
March 14 March 10 April 11
April 25 April 21 May 23
June 6 June 2 July 4
July 18 July 14 August 15
August 29 August 25 September 26
October 10 October 6 November 7
November 28 November 22 December 26
 

2017 nhrMAX, tkMAX, and pathMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing

nhrMAX,
tkMAX, pathMAX

February 14 February 10 March 14
March 28 March 24 April 25
May 9 May 5 June 6
June 20 June 16 July 18
August 1 July 28 August 29
September 12 September 8 October 10
October 24 October 20 November 21