Activity-based ABL1 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ABL1
Enzyme
Human ABL1
HGNC
ABL1
Synonym
Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
| Mutant | Staurosporine | PP2 | AG1478 | PDGFR I-III | D-64406 |
|---|---|---|---|---|---|
| WT | 60 | 140 | 540 | n.a. | 670 |
| G250E | 22 | 207 | 525 | n.a. | 507 |
| Q252H | 25.9 | 56.7 | 321 | n.a. | 635 |
| Y253F | 48.2 | 51.8 | 285 | 58,500 | 267 |
| Y253H | 27 | 68 | 220 | >100,000 | 255 |
| E255K | 140 | 435 | 830 | n.a. | 870 |
| E255V | 43 | 90 | 220 | >100,000 | 310 |
| V299L | 58 | 2.0 | 60 | >100,000 | 290 |
| T315I | 24.2 | n.a. | 2,400 | n.a. | 2,600 |
| F317I | 78 | 51 | 420 | >100,000 | 3,700 |
| F317L | 150 | 45 | 180 | >100,000 | 1,100 |
| M351T | 50.3 | 104 | 346 | 665,000 | 418 |
| H396P | 46.3 | 71.5 | 317 | >126,000 | 510 |
Screening Location
Malvern, USA