ALK Kinase Mutant Profiler Service

Activity-based ALK mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#

ALK

Enzyme

Human ALK

HGNC

ALK

Synonym

ALK tyrosine kinase receptor [Precursor], Anaplastic lymphoma kinase

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 2.3 n.a. 16,300 n.a. n.a. n.a.
T1151-L1152insT 2.5 44,000 3,600 >100,000 n.a. 33,000
T1151M 1.7 3,900 460 >100,000 n.a. 13,000
L1152R 1.9 12,000 1,000 >100,000 n.a. 12,000
C1156Y 2.6 18,000 3,700 >100,000 n.a. 18,000
F1174L 3.3 16,000 2,600 >100,000 n.a. 20,000
F1174L-EML4 5.4 12,000 2,800 >100,000 n.a. 88,000
F1174-NPM1 4.9 19,000 1,940 >100,000 n.a. 56,000
F1174S 2.5 2,600 210 >100,000 n.a. 19,000
L1196M 0.9 >20,000 8,000 >20,000 n.a. >20,000
G1202R 4.0 3,100 2,100 >100,000 n.a. 33,000
S1206R 1.0 10,000 690 >100,000 n.a. 17,000
G1269A 1.3 45,000 3,000 >100,000 n.a. 9,000
G1269S 1.3 >100,000 6,900 >100,000 n.a. 42,000
R1275Q 2.3 12,000 1,100 >100,000 n.a. 20,000
KIF5B 9.5 >100,000 3,900 n.a. >100,000 27,000
KLC1 6.81 >100,000 3,000 n.a. >100,000 28,000
NPM1 5.5 19,000 2,800 >100,000 n.a. 35,000
TFG 3.7 11,600 2,200 >50,000 n.a. 28,000
TFG (Tex4Aex20) 3.9 >100,000 3,000 n.a. >100,000 27,500
TPM1 2.3 62,000 2,500 n.a. >100,000 35,000
TPM3 2.9 15,000 1,600 >100,000 n.a. 34,000
Screening Location

Malvern, USA