Activity-based RET mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
RET
Enzyme
Human RET
HGNC
RET
Synonym
Proto-oncogene tyrosine-protein kinase receptor ret [Precursor], C-ret
Scientific Information
P07949 (http://www.uniprot.org/uniprot/P07949)
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 | 7.1 | 24 | 260 | n.a. | >100,000 | 104 |
| G691S | 4.3 | 20 | 280 | n.a. | >100,000 | 180 |
| R749T | 4.9 | 17 | 230 | n.a. | >100,000 | 130 |
| E762Q | 8.0 | 28 | 480 | n.a. | >100,000 | 260 |
| V778I | 5.2 | 36 | 500 | n.a. | >100,000 | 250 |
| L790F | 15 | 13 | 140 | n.a. | >100,000 | 330 |
| Y791F | 9.8 | 37 | 34 | n.a. | >100,000 | 240 |
| V804E | 2.3 | 9,200 | 28,000 | n.a. | >100,000 | 400 |
| V804L | 2.2 | >100,000 | >100,000 | n.a. | >100,000 | 540 |
| V804L-KIF5B | 1.7 | >100,000 | >100,000 | n.a. | >100,000 | 350 |
| V804M | 0.3 | 4,100 | 11,000 | n.a. | >100,000 | 150 |
| V804M-KIF5B | 1.4 | >100,000 | >100,000 | n.a. | >100,000 | 320 |
| Y806H | 8.0 | 78 | 1,900 | n.a. | >100,000 | 790 |
| G810C | 260 | 50 | 15,300 | n.a. | >100,000 | 3,600 |
| G810R | 460 | 35 | 21,700 | n.a. | >100,000 | 5,800 |
| G810S | 340 | 240 | 6,700 | n.a. | >100,000 | 4,100 |
| R813Q | 3.9 | 6.7 | 120 | n.a. | >100,000 | 120 |
| A883F | 6.2 | 10 | 140 | n.a. | >100,000 | 440 |
| S891A | 1.0 | 26 | 110 | n.a. | >100,000 | 73 |
| S904A | 6.3 | 21 | 200 | n.a. | >100,000 | 110 |
| S904F | 7.7 | 27 | 310 | n.a. | >100,000 | 120 |
| R912P | 5.2 | 24 | 260 | n.a. | >100,000 | 130 |
| M918T | 4.3 | 21 | 290 | n.a. | >100,000 | 130 |
| BCR | 6.2 | 31 | 510 | n.a. | >100,000 | 140 |
| CCDC6-PTC1 | 5.1 | 28 | 450 | n.a. | >100,000 | 140 |
| KIF5B-Kex15Rex14 | 4.3 | 23 | 290 | n.a. | >100,000 | 115 |
| NCOA4-PTC3 | 5.0 | 27 | 330 | n.a. | >100,000 | 160 |
| PRKAR1A-PTC2 | 3.8 | 33 | 320 | n.a. | >100,000 | 120 |
| E732K | 6.0 | 30 | 610 | n.a. | >100,000 | 220 |
| L730I | 190 | 120 | 5,000 | n.a. | >100,000 | 1,500 |
| L730M | 43 | 20 | 360 | n.a. | >100,000 | 270 |
| V738A | 30 | 410 | 3,700 | n.a. | >100,000 | 1,000 |
| Y806C | 110 | 110 | 2,100 | n.a. | >100,000 | 1,000 |
| Y806N | 80 | 130 | 6,900 | n.a. | >100,000 | 2,200 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
PDF