TIE Kinase Mutant Profiler Service

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

TIE2

Enzyme

Human TIE2

HGNC

TEK

Synonym

Angiopoietin-1 receptor [Precursor], Tyrosine-protein kinase receptor TIE-2, hTIE2, Tyrosine-protein kinase receptor TEK, p140 TEK, Tunica interna endothelial cell 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 D-64406
WT 11.2 4,400 6,700 n.a. 5,300
A1124V 37 5,400 13,000 35,000 21,000
P883A 39 4,200 6,600 24,000 30,000
R849W 15 6,300 15,000 >100,000 >100,000
Y1108F 16 12,000 17,000 >100,000 >100,000
Y897C 120 19,000 26,000 >100,000 >100,000
Y897S 190 >100,000 >100,000 >100,000 >100,000
Screening Location

Malvern, USA