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| | LanthaScreen TR-FRET Assay |
| Description: | Compound 1 was also assayed to determine the IC50 values for three different kinases (PCTAIRE1, DYRK1a, and CDK2) in comparison to Gsk3beta. The assay was conducted with the same method described below in the second assay. Activity on human GSK-3beta was assessed using the following methods (according to Meijer et al., Chem. Biol., 2003-10:1255-1266). In a first screening assay, compounds were tested in duplicate at a concentration of 10 M.Human recombinant enzyme GSK-3beta was incubated for 90 minutes at 22° C. in the presence of compounds or vehicle in a reaction buffer containing ATP plus 100 nM unphosphorylated specific substrate peptide (Ulight-CFFKNIVTPRTPPPSQGK-amide). Substrate phosphorylation was measured by LANCE technology (PerkinElmer, Conn., USA). The results, reported in the following Table 4, are expressed as a percent of inhibition of control specific activity obtained in the presence of the test compounds (as % inhibition at 10 um). |
| Affinity data for this assay | |
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