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. 2017 Aug 8;7:7501. doi: 10.1038/s41598-017-07755-y

Figure 2.

Figure 2

DSF screening identified few hit compounds for active VRKs. Heat maps showing DSF screening data for (a) VRK1, (b) VRK2 and (c) AAK1 (included for comparison) versus a 378-compound library of cell-permeable, bioactive kinase inhibitors. The color scheme is the same as in Fig. 1a. Panels indicate rows (x-axis) and lines (y-axis) in a 384-well plate. Numbers show the observed ΔTm shift in degrees Celsius. (d) Bar graph showing ΔTm (°C) for top hit compounds for VRK1 (blue bars) and VRK2 (orange bars). (e) The three compounds used in crystallization. BI-D1870 was used as a racemic mix; the chiral carbon is marked with a star.