Activity-based TRKC mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
TRKC
Enzyme
Human TRKC
HGNC
NTRK3
Synonym
NT-3 growth factor receptor [Precursor], Neurotrophic tyrosine kinase receptor type 3, TrkC tyrosine kinase, GP145-TrkC, NTRK3
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 | D-64406 |
|---|---|---|---|---|---|---|
| WT | <0.1 | 3,000 | 3,800 | 6,900 | n.a. | 321 |
| G623E | 15 | 6,400 | >100,000 | n.a. | >100,000 | >100,500 |
| G623R | 19 | 49,100 | >100,000 | n.a. | >100,000 | >100,000 |
| G623R/L686M | 113 | >100,000 | >100,000 | n.a. | >100,000 | 38,000 |
| L686M | 11 | 22,000 | >100,000 | n.a. | >100,000 | 2,600 |
| G696A | 0.9 | 9,800 | 14,000 | n.a. | >100,000 | 220 |
Screening Location
Malvern, USA
PDF