Activity-based ALK mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ALK
Enzyme
Human ALK
HGNC
ALK
Synonym
ALK tyrosine kinase receptor [Precursor], Anaplastic lymphoma kinase
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 | 2.3 | n.a. | 16,300 | n.a. | n.a. | n.a. |
| C1156Y | 2.6 | 18,000 | 3,700 | >100,000 | n.a. | 18,000 |
| EML4 (Eex14Aex20) | 3.2 | 18,000 | 1,900 | n.a. | >100,000 | 31,000 |
| EML4 (Eex6Aex20) | 2.3 | 13,000 | 1,300 | n.a. | >100,000 | 19,000 |
| EML4 (Eex13Aex20) | 3.3 | 23,000 | 2,600 | n.a. | >100,000 | 27,000 |
| EML4 (Eex20Aex20) | 4.0 | 24,000 | 1,700 | n.a. | >100,000 | 25,000 |
| F1174L | 3.3 | 16,000 | 2,600 | >100,000 | n.a. | 20,000 |
| F1174L-EML4 | 5.4 | 12,000 | 2,800 | >100,000 | n.a. | 88,000 |
| F1174-NPM1 | 4.9 | 19,000 | 1,940 | >100,000 | n.a. | 56,000 |
| F1174S | 2.5 | 2,600 | 210 | >100,000 | n.a. | 19,000 |
| G1202R | 4.0 | 3,100 | 2,100 | >100,000 | n.a. | 33,000 |
| G1269A | 1.3 | 45,000 | 3,000 | >100,000 | n.a. | 9,000 |
| G1269S | 1.3 | >100,000 | 6,900 | >100,000 | n.a. | 42,000 |
| I1171N/D1203N | 36 | 33,700 | >100,000 | n.a. | >100,000 | n.a. |
| KIF5B | 9.5 | >100,000 | 3,900 | n.a. | >100,000 | 27,000 |
| KLC1 | 6.81 | >100,000 | 3,000 | n.a. | >100,000 | 28,000 |
| L1152R | 1.9 | 12,000 | 1,000 | >100,000 | n.a. | 12,000 |
| L1196M | 0.9 | >20,000 | 8,000 | >20,000 | n.a. | >20,000 |
| L1196M/G1202R | 1.0 | 4,200 | 6,000 | n.a. | >100,000 | 33,000 |
| NPM1 | 5.5 | 19,000 | 2,800 | >100,000 | n.a. | 35,000 |
| R1275Q | 2.3 | 12,000 | 1,100 | >100,000 | n.a. | 20,000 |
| S1206R | 1.0 | 10,000 | 690 | >100,000 | n.a. | 17,000 |
| STRN (Sex3Aex20) | 1.0 | 9,800 | 910 | n.a. | >100,000 | 16,000 |
| T1151-L1152insT | 2.5 | 44,000 | 3,600 | >100,000 | n.a. | 33,000 |
| T1151M | 1.7 | 3,900 | 460 | >100,000 | n.a. | 13,000 |
| TFG | 3.7 | 11,600 | 2,200 | >50,000 | n.a. | 28,000 |
| TFG (Tex4Aex20) | 3.9 | >100,000 | 3,000 | n.a. | >100,000 | 27,500 |
| TPM1 | 2.3 | 62,000 | 2,500 | n.a. | >100,000 | 35,000 |
| TPM3 | 2.9 | 15,000 | 1,600 | >100,000 | n.a. | 34,000 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays.
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