Assay Method Information

Assay Name:  Kinase Inhibition Assay
Description:  2.5 times of the kinase (VEGFR2 or EGFR or FYN) buffer solution was added to the compound diluted in equal concentration in the 384-well plate and incubated at 22-27° C. for 10 minutes, then 2.5 times of the FAM-labeled peptide substrate and ATP buffer solution were added therein and incubated at 28° C., and then the stop buffer solution was added to stop the reaction. The data was read by Caliper and the following formula was used to calculate the IC50 inhibition: Percent inhibition=(max-conversion)/(max-min)*100. Staurosporine was used as a control. In kinase inhibition assays, some of the compounds of the present invention are effective in inhibiting VEGFR2/FYN/EGFR, so they have the potential for treating or preventing cancer or central nervous system diseases (Table 1).
Affinity data for this assay
 

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