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