c-MET Kinase Mutant Profiler Service

Activity-based c-MET mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.

Target Overview
CAT#

c-MET

Enzyme

Human c-MET

HGNC

MET

Synonym

Hepatocyte growth factor receptor [Precursor], HGF receptor, Scatter factor receptor, SF receptor, HGF/SF receptor, Met proto-oncogene tyrosine kinase, c-Met, MET

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 260 >20,000 4,800 >20,000 n.a. 13,000
P991S 240 >100,000 >100,000 >100,000 n.a. 20,000
T992I 250 >100,000 7,500 >100,000 n.a. 36,000
V1092I 260 >100,000 19,000 >100,000 n.a. >50,000
H1094L 190 >100,000 12,000 n.a. >100,000 19,000
H1094Y 500 >100,000 17,000 n.a. >100,000 14,000
G1163R 2,100 >100,000 11,000 n.a. >100,000 42,000
T1173I 120 >100,000 12,500 >100,000 n.a. 50,000
L1195F 160 >100,000 28,000 n.a. >100,000 27,000
L1195V 200 >100,000 >100,000 n.a. >100,000 11,000
F1200I 120 >100,000 >100,000 53,000 n.a. 24,000
D1228A 190 >100,000 12,500 n.a. >100,000 26,000
D1228G 210 >100,000 16,000 n.a. >100,000 15,000
D1228H 56 >100,000 11,000 27,000 n.a. 25,000
D1228N 44 >100,000 34,000 37,000 n.a. 21,000
D1228V 85 >100,000 12,000 n.a. >100,000 19,000
D1228Y 120 >100,000 27,000 n.a. >100,000 22,000
Y1230A 83 >100,000 9,000 20,000 n.a. 36,000
Y1230C 50 >100,000 6,800 31,000 n.a. 29,000
Y1230D 30 >100,000 2,800 40,000 n.a. 12,000
Y1230H 62 >100,000 10,000 27,000 n.a. 26,000
Y1230S 230 >100,000 10,600 n.a. >100,000 29,000
Y1235D 140 >100,000 15,000 >100,000 n.a. 36,000
K1244R 280 >100,000 6,100 n.a. >100,000 21,000
M1250I 250 >100,000 13,500 n.a. >100,000 17,000
M1250T 338 n.a. 45,500 n.a. n.a. 26,500
KIF5B 140 >100,000 9,600 n.a. >100,000 17,000
TFG 180 >100,000 7,500 n.a. >100,000 21,000
Screening Location

Malvern, USA