| Assay Method Information | |
| | DYRK2 Kinase Activity Analysis and Detection Method |
| Description: | The DYRK2 kinase inhibitory activity of the compounds of the invention were measured. The method was briefly described as follows (for specific methods, see Banerjee S, Wei T, Wang J, et al. Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression[J]. Proceedings of the National Academy of Sciences, 2019, 116(49): 24881-24891): 1) Compounds with different concentrations were added into a 384-well plate, and re-dissolved, followed by the addition of DYRK2 protein, the substrate Woodtide (KKISGRLSPIMTEQ) and 33P-γATP, and the mixture were mixed evenly. 2) The mixture was incubated for 30 minutes at room temperature.3) 0.5 M (3%) orthophosphoric acid solution was added to terminate the reaction, and then the mixture was transferred to P81 plate and washed with 50 mM orthophosphoric acid solution. 4) IC50 results were calculated using GraphPad Prism software. |
| Affinity data for this assay | |
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