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 Name | Entrez Gene Symbol |
| c-KIT | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT) | c-KIT |
| c-Ret-GFRα2 | Proto-oncogene tyrosine-protein kinase receptor Ret (RET) | c-Ret-GFRα2 |
| DDR1 | Discoidin domain receptor 1 (CD167a) | DDR1 |
| EphA5 | Ephrin type-A receptor 5 (EphA5) | EphA5 |
| EphA7 | Ephrin type-A receptor 7 (EphA7) | EphA7 |
| EphB2 | Ephrin type-B receptor 2 (EphB2) | EphB2 |
| EphB3 | Ephrin type-B receptor 3 (EphB3) | EphB3 |
| EphB4 | Ephrin type-B receptor 4 (EphB4) | EphB4 |
| ErbB1 | v-erb-b2 erythroblastic leukemia viral oncogene homolog 1 (EGFR) | ErbB1 |
| ErbB2-ErbB3 | v-erb-b2 erythroblastic leukemia viral oncogene homolog 2 (HER2) | ErbB2-ErbB3 |
| ErbB4 | erb-b2 receptor tyrosine kinase 4 | ErbB4 |
| FGR | FGR proto-oncogene, Src family tyrosine kinase (FGR) | FGR |
| FLT4 | fms-related tyrosine kinase 4 (FLT4) | FLT4 |
| IGF1R | Insulin-like growth factor 1 receptor (IGF1R) | IGF1R |
| INSRb | Insulin receptor, isoform B (INSR) | INSRb |
| JAK3 | Janus kinase 3 (JAK3) | JAK3 |
| KDR | Kinase Insert Domain Receptor (VEGFR2) | KDR |
| PDGFRa | Platelet-derived growth factor receptor alpha (PDGFRa) | PDGFRa |
| PDGFRb | Platelet-derived growth factor receptor beta (PDGFRb) | PDGFRB |
| PRLR-JAK1 | Prolactin receptor (PRLR) | PRLR-JAK1 |
| PRLR-JAK2 | Prolactin receptor (PRLR) | PRLR-JAK2 |
| TrkA-P75 | Neurotrophic tyrosine kinase receptor type 1 (NTRK1) | TrkA-P75 |
| TrkB-P75 | Neurotrophic tyrosine kinase receptor type 2 (NTRK2) | TrkB-P75 |
| TrkC-P75 | Neurotrophic tyrosine kinase receptor type 3 (NTRK3) | TrkC-P75 |
| TYK2 | Tyrosine 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:
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 |