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tkE/IC50ELECT

Quantitate compound potency against any TKscanSM functional cell-based assay. Agonist half maximal effective concentrations (EC50s) and antagonist half maximal inhibitory concentrations (IC50s) are calculated from duplicate 10-point dose-response curves. Measurements are made under optimized conditions to generate consistent and reproducible data that reliably reflects the drug's potency.

tkE/IC50ELECT may be used as an ideal follow-up study tool to quantify the potency of compound-kinase target interactions identified in primary screens, to supplement existing data, or support lead optimization and SAR activity.

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Panel Features & Benefits

  • 10-point dose response curve in duplicate
  • Choose from 34 RTK and CTK assays
  • High quality reproducible data
  • Inhibitor and agonist mode – identify small molecule inhibitors and/or antibody therapeutics
  • Rapid turnaround time
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).

tkE/IC50ELECT 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
FGFR2Epidermal growth factor receptor (EGFR)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 

What does the term EC50 mean?

The term half maximal effective concentration (EC50) refers to the concentration of a drug or biologic which induces a response halfway between the baseline and the maximum. Therefore, the EC50 of a compound or biologic represents the concentration where 50% of it’s maximal effect can be observed. It is commonly used as a measure of the drug’s potency.

What does an IC50 measure?

The term half maximal inhibitory concentration (EC50) is a measure of the effectiveness of a compound to inhibit a given biological response. Therefore, the IC50 of a compound or biologic represents the half maximal (50%) inhibitory concentration and is commonly used as a measure of antagonist drug’s potency.

How are the EC50/IC50s calculated?

For each compound/GPCR target interaction, dose response curves  are generated using 10 concentrations of agonist or antagonist (10-point curve). The results are reported as EC50/IC50 which derived using the Hill equation:

hill equation