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
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 | 1.2 | 21 | 350 | >20,000 | n.a. | 250 |
| G691S | 1.1 | 8.2 | 185 | 18,000 | n.a. | 240 |
| R749T | 2.0 | 5.5 | 140 | 2,600 | n.a. | 48 |
| E762Q | 1.5 | 20 | 380 | 26,000 | n.a. | 350 |
| V778I | 5.0 | 4.0 | 82 | 16,600 | n.a. | 66 |
| L790F | 5.1 | 1.4 | 39 | 10,000 | n.a. | 78 |
| Y791F | 0.5 | 5.2 | 94 | 10,000 | n.a. | 230 |
| V804E | 4.2 | 3,100 | 9,200 | 12,000 | n.a. | 420 |
| V804L | 4.9 | 84,000 | 130,000 | n.a. | n.a. | 1,900 |
| V804L-KIF5B | 1.1 | >100,000 | 48,000 | n.a. | >100,000 | 310 |
| V804M | 0.53 | 11,600 | 47,000 | 29,400 | n.a. | 561 |
| V804M-KIF5B | 2.8 | >100,000 | 31,000 | n.a. | >100,000 | 340 |
| Y806H | 4.7 | 17 | 850 | >100,000 | n.a. | 340 |
| 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 | 1.0 | 4.8 | 150 | 12,000 | n.a. | 260 |
| A883F | 9.6 | 4.0 | 75 | 19,600 | n.a. | 550 |
| S891A | 2.6 | 3.5 | 26 | 8,500 | n.a. | 16 |
| S904A | 3.5 | 11 | 230 | 12,000 | n.a. | 55 |
| S904F | 2.3 | 9.0 | 150 | 13,000 | n.a. | 130 |
| R912P | 3.6 | 9.3 | 210 | n.a. | >100,000 | 103 |
| M918T | 1.0 | 15 | 340 | 26,000 | n.a. | 360 |
| BCR | 2.2 | 13 | 160 | 15,700 | n.a. | 120 |
| CCDC6-PTC1 | 3.4 | 4.2 | 51 | 17,000 | n.a. | 41 |
| KIF5B-Kex15Rex14 | 11 | 6.8 | 120 | n.a. | >100,000 | 72 |
| NCOA4-PTC3 | 4.5 | 4.2 | 72 | 18,000 | n.a. | 74 |
| PRKAR1A-PTC2 | 4.4 | 3.7 | 91 | 27,000 | n.a. | 54 |
Screening Location
Malvern, USA