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DYRK1A binding correlates to DYRK-NFAT EC50 and β-cell replication, while MELK binding does not correlate to cytotoxicity. (A) Selected compounds (5, 15, 21, 28, and 42) for which DYRK-NFAT EC50 was linear with DYRK1A Kd (R2=0.98) plotted as DYRK-NFAT EC50 vs DYRk1A Kd. (B) The same compounds (5, 15, 21, 28, and 42) with R-Luc CC50 plotted versus MELK Kd (R2=0.05). (C) The same compounds (5, 15, 21, 28, and 42) with human β-cell replication ECmin plotted versus DYRK1A Kd (R2=0.99).
