Activity-based TRKA mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
TRKA
Enzyme
Human TRKA
HGNC
NTRK1
Synonym
High affinity nerve growth factor receptor [Precursor], Neurotrophic tyrosine kinase receptor type 1, TRK1 transforming tyrosine kinase protein, p140-TrkA, NTRK1
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
| Mutant | Staurosporine | PP2 | AG1478 | PDGFR I-III | EGFR/ErbB Inhibitor | EMD 324840 | D-64406 |
|---|---|---|---|---|---|---|---|
| WT | 3.0 | 16,000 | n.a. | n.a. | n.a. | 2,300 | |
| F589L | 0.34 | >100,000 | 36,000 | n.a. | >100,000 | n.a. | 410 |
| G595R | 12 | 44,000 | >100,000 | n.a. | n.a. | >100,000 | 36,000 |
| G595R/A608D | 2.7 | 6,800 | >100,000 | n.a. | >100,000 | n.a. | 6,700 |
| G595R/L657M | 10 | >100,000 | >100,000 | n.a. | >100,000 | n.a. | 14,000 |
| G595R/G667A | 1.2 | 3,900 | >100,000 | n.a. | >100,000 | n.a. | 13,000 |
| G595R/G667C | 1.1 | 6,400 | >100,000 | n.a. | >100,000 | n.a. | 11,000 |
| G595R/G667S | 1.2 | 6,500 | >100,000 | n.a. | >100,000 | n.a. | 16,200 |
| A608D | 2.40 | >100,000 | 36,000 | n.a. | >100,000 | n.a. | 650 |
| L657M | 0.67 | >100,000 | 28,000 | n.a. | >100,000 | n.a. | 2,300 |
| G667C | 0.47 | 1,900 | 9,000 | 560 | n.a. | n.a. | 46 |
| G667S | 0.06 | 1,100 | 3,200 | n.a. | >100,000 | n.a. | 790 |
| TFG | 0.24 | 740 | 2,500 | 3,300 | n.a. | n.a. | 190 |
| TPM3 | 0.2 | 480 | 2,800 | 2,500 | n.a. | n.a. | 77 |
| TPR | 0.3 | 670 | 2,400 | 1,800 | n.a. | n.a. | 76 |
Screening Location
Malvern, USA
PDF