Fig. 1.
DYRK1A kinase pilot screening of the Prestwick chemical compound set. An automated TR-FRET assay for DYRK1A using an optimized LanthaScreen® Eu Kinase Binding Assay for low volume in 384-well format was used to screen the Prestwick collection (at 6.7 μM). The scatterplot shows percent inhibition for the Prestwick set compounds (black circles), negative inhibition controls (DMSO; red inverted triangles), and positive inhibition controls (6.7 μM harmine; blue triangles). Compounds showing ≥ 50% inhibition (dotted red line) were selected for confirmation. β-carbolines are highlighted with red circles.