ABL1 Kinase Mutant Profiler Service

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