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 |
| D1213H | 43 | >100,000 | 35,500 | n.a. | >100,000 | 8,600 |
| D1228A | 24 | >100,000 | 21,500 | n.a. | >100,000 | 12,000 |
| D1228G | 32 | >100,000 | 33,000 | n.a. | >100,000 | 10,000 |
| D1228H | 27 | >100,000 | 17,000 | n.a. | >100,000 | 9,300 |
| D1228N | 24 | >100,000 | 26,500 | n.a. | >100,000 | 9,900 |
| D1228V | 12 | >100,000 | 20,500 | n.a. | >100,000 | 11,000 |
| D1228Y | 29 | >100,000 | 52,000 | n.a. | >100,000 | 47,000 |
| DelEx14 | 22 | >100,000 | 21,000 | n.a. | >100,000 | 15,000 |
| F1200I | 34 | >100,000 | >100,000 | n.a. | >100,000 | 13,000 |
| G1163R | 590 | >100,000 | 32,000 | n.a. | >100,000 | 75,000 |
| H1094L | 49 | >100,000 | >100,000 | n.a. | >100,000 | 20,000 |
| H1094Y | 70 | >100,000 | >100,000 | n.a. | >100,000 | 8,800 |
| K1244R | 21 | >100,000 | 20,000 | n.a. | >100,000 | 16,000 |
| KIF5B | 22 | >100,000 | 17,000 | n.a. | >100,000 | 14,000 |
| L1195F | 8.3 | >100,000 | 16,000 | n.a. | >100,000 | 9,300 |
| L1195V | 31 | >100,000 | 66,000 | n.a. | >100,000 | 9,300 |
| M1250I | 25 | >100,000 | 19,000 | n.a. | >100,000 | 9,700 |
| M1250T | 59 | >100,000 | 41,000 | n.a. | >100,000 | 15,000 |
| P991S | 24 | >100,000 | 23,000 | n.a. | >100,000 | 17,000 |
| R1227K | 40 | >100,000 | 13,000 | n.a. | >100,000 | 21,000 |
| R970C | 20 | >100,000 | 17,000 | n.a. | >100,000 | 18,000 |
| T1173I | 21 | >100,000 | 25,000 | n.a. | >100,000 | 15,000 |
| T992I | 27 | >100,000 | 26,000 | n.a. | >100,000 | 17,000 |
| TFG | 38 | >100,000 | 16,000 | n.a. | >100,000 | 13,000 |
| V1092I | 50 | >100,000 | 24,000 | n.a. | >100,000 | 40,000 |
| WT | 34 | >100,000 | 8,100 | n.a. | >100,000 | 11,000 |
| Y1230A | 25 | >100,000 | 50,000 | n.a. | >100,000 | 14,000 |
| Y1230C | 26 | >100,000 | 27,000 | n.a. | >100,000 | 15,000 |
| Y1230D | 13 | >100,000 | 17,000 | n.a. | >100,000 | 12,000 |
| Y1230H | 22 | >100,000 | 39,000 | n.a. | >100,000 | 17,000 |
| Y1230S | 25 | >100,000 | >100,000 | n.a. | >100,000 | 18,000 |
| Y1235D | 40 | >100,000 | 16,000 | n.a. | >100,000 | 21,000 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
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