TRKA Kinase Mutant Profiler Service

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

TRKA

Enzyme

Human TRKA

HGNC

NTRK1

Synonym

High affinity nerve growth factor receptor [Precursor], Neurotrophic tyrosine kinase receptor type 1, TRK1 transforming tyrosine kinase protein, p140-TrkA, NTRK1

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 EMD 324840 D-64406
WT 3.0 16,000 n.a. n.a. n.a. 2,300
F589L 0.34 >100,000 36,000 n.a. >100,000 n.a. 410
G595R 12 44,000 >100,000 n.a. n.a. >100,000 36,000
G595R/A608D 2.7 6,800 >100,000 n.a. >100,000 n.a. 6,700
G595R/L657M 10 >100,000 >100,000 n.a. >100,000 n.a. 14,000
G595R/G667A 1.2 3,900 >100,000 n.a. >100,000 n.a. 13,000
G595R/G667C 1.1 6,400 >100,000 n.a. >100,000 n.a. 11,000
G595R/G667S 1.2 6,500 >100,000 n.a. >100,000 n.a. 16,200
A608D 2.40 >100,000 36,000 n.a. >100,000 n.a. 650
L657M 0.67 >100,000 28,000 n.a. >100,000 n.a. 2,300
G667C 0.47 1,900 9,000 560 n.a. n.a. 46
G667S 0.06 1,100 3,200 n.a. >100,000 n.a. 790
TFG 0.24 740 2,500 3,300 n.a. n.a. 190
TPM3 0.2 480 2,800 2,500 n.a. n.a. 77
TPR 0.3 670 2,400 1,800 n.a. n.a. 76
Screening Location

Malvern, USA