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tkELECTSM - Personalized Screening & Profiling

Customized compound profiling using our expanding menu of tyrosine kinase assays. Choose from a large collection of whole cell, functional assays that monitor the activity of a specific receptor tyrosine kinase (RTK) or cytosolic tyrosine kinase (CTK) by measuring the tyrosine phosphorylation status of proteins in their natural cellular environment. tkELECT is a flexible solution with multiple applications including, primary HTS & lead discovery and ongoing lead optimization & SAR and is ideal for identifying novel receptor tyrosine kinase inhibitors, allosteric modulators or antibody therapeutics.

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Panel Features & Benefits

  • Customized screening and profiling - choose from 34 RTK and CTK assays
  • High quality reproducible data
  • Flexible - standardized or custom panels
  • Inhibitor and agonist mode – identify small molecule inhibitors and/or antibody therapeutics
  • Broad applications – including specificity and compound liability
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 assays 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 serious 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).

tkELECT Assay Panel

Listed below are the assays currently available for screening and profiling.

 
Gene Symbol ▲Kinase NameEntrez Gene Symbol
AXLAXL receptor tyrosine kinase (AXL)AXL
BLKB lymphoid tyrosine kinase (BLK)BLK
BTKBruton agammaglobulinemia tyrosine kinase (BTK)BTK
cINSRaInsulin receptor, isoform A (INSR)cINSRa
cINSRbInsulin receptor, isoform B (INSR)cINSRb
c-KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT)c-KIT
CLK1CDC-Like Kinase 1 (CLK1)CLK1
CLK2CDC-Like Kinase 2 (CLK2)CLK2
c-Ret-GFRα1Proto-oncogene tyrosine-protein kinase receptor Ret (RET)c-Ret-GFRα1
c-Ret-GFRα2Proto-oncogene tyrosine-protein kinase receptor Ret (RET)c-Ret-GFRα2
CSF1Rcolony-stimulating factor 1 receptor (CSF1R)CSF1R
CSF3R-JAK1colony stimulating factor 3 receptor (CSF3R-JAK1)CSF3R-JAK1
CSNK1Dcasein kinase 1, delta (CSNK1D)CSNK1D
DDR1Discoidin domain receptor 1 (CD167a)DDR1
EGFR/ErbB3Epidermal growth factor receptorEGFR
EphA4EPH receptor A4 (EphA4)EphA4
EphA5Ephrin type-A receptor 5 (EphA5)EphA5
EphA7Ephrin type-A receptor 7 (EphA7)EphA7
EphB1Ephrin type-B receptor 1 (EphB1)EphB1
EphB2Ephrin type-B receptor 2 (EphB2)EphB2
EphB3Ephrin type-B receptor 3 (EphB3)EphB3
EphB4Ephrin type-B receptor 4 (EphB4)EphB4
EpoR-JAK2Erythropoietin receptor (EpoR)EpoR-JAK2
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
FGFR1Fibroblast growth factor receptor 1 (FGFR1)FGFR1
FGFR1-α-KlothoFibroblast Growth Factor Receptor 1 (FGFR1), α-KlothoFGFR1-α-Klotho
FGFR1-β-KlothoFibroblast growth factor receptor 1 (FGFR1), β-KlothoFGFR1-β-Klotho
FGFR2Fibroblast growth factor receptor 2 (FGFR2)FGFR2
FGFR4Fibroblast growth factor receptor 4 (FGFR4)FGFR4
FGFR4-α-KlothoFibroblast Growth Factor Receptor 4 (FGFR4), α-KlothoFGFR4-α-Klotho
FGFR4-β-KlothoFibroblast growth factor receptor 4 (FGFR4), β-KlothoFGFR4-β-Klotho
FGRFGR proto-oncogene, Src family tyrosine kinase (FGR)FGR
FLT4fms-related tyrosine kinase 4 (FLT4)FLT4
GHR-JAK1Growth hormone receptor (GHR-JAK1)GHR-JAK1
GHR-JAK2Growth hormone receptor (GHR-JAK2)GHR-JAK2
HCKHemopoietic cell kinase (HCK)HCK
IGF1RInsulin-like growth factor 1 receptor (IGF1R)IGF1R
INSRaInsulin receptor, isoform A (INSR)INSRa
INSRbInsulin receptor, isoform B (INSR)INSRb
JAK3Janus kinase 3 (JAK3)JAK3
KDRKinase Insert Domain Receptor (VEGFR2)KDR
MEK1Mitogen-activated protein kinase kinase 1 (MAP2K1)MEK1
mINSRaInsulin receptor, isoform A (INSR)mINSRa
mINSRbInsulin receptor, isoform B (INSR)mINSRb
PDGFRaPlatelet-derived growth factor receptor alpha (PDGFRa)PDGFRa
PDGFRbPlatelet-derived growth factor receptor beta (PDGFRb)PDGFRB
PI3KδPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta)PI3Kδ
PIM1Pim-1 oncogene (PIM1)PIM1
PRLR-JAK1Prolactin receptor (PRLR)PRLR-JAK1
PRLR-JAK2Prolactin receptor (PRLR)PRLR-JAK2
PYK2PTK2B protein tyrosine kinase 2 beta (PTK2B)PYK2
rhTrkA-rhP75Neurotrophic tyrosine kinase receptor type 1 (NTRK1)rhTrkA-rhP75
RIPK1Receptor (TNFRSF)-Interacting Serine-Threonine Kinase 1 (RIPK1)RIPK1
RIPK2Receptor-interacting serine-threonine kinase 2 (RIPK2)RIPK2
RIPK3Receptor-Interacting Serine-Threonine Kinase 3 (RIPK3)RIPK3
rTrkA-rP75Neurotrophic tyrosine kinase receptor type 1 (NTRK1)rTrkA-rP75
SIK1Salt-inducible kinase 1 (SIK1)SIK1
SYKSpleen tyrosine kinase (SYK)SYK
Tie2Angiopoietin-1 receptor (Tie2)Tie2
TrkANeurotrophic tyrosine kinase receptor type 1 (NTRK1)TrkA
TrkA-P75Neurotrophic tyrosine kinase receptor type 1 (NTRK1)TrkA-P75
TrkBNeurotrophic tyrosine kinase receptor type 2 (NTRK2)TrkB
TrkB-P75Neurotrophic tyrosine kinase receptor type 2 (NTRK2)TrkB-P75
TrkCNeurotrophic tyrosine kinase receptor type 3 (NTRK3)TrkC
TrkC-P75Neurotrophic tyrosine kinase receptor type 3 (NTRK3)TrkC-P75
TYK2Tyrosine kinase 2 (TYK2)TYK2
YES1v-yes-1 Yamaguchi sarcoma viral oncogene homolog 1 (YES)YES1

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