Figure 1 | Scientific Reports

Figure 1

From: Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

Figure 1

Analysis of published thermal shift assay (DSF) screening data for VRK1-PKIS. (a) Heat map showing DSF screening data for PKIS compounds with ΔTm > 2.0 °C for VRK1 (black box) together with the results for other 67 kinases (x-axis). Compounds were ranked (top to bottom) according to decreasing ΔTm for VRK1. Background color indicates ΔTm as a gradient from 2.0 °C (yellow) to the maximum observed ΔTm for each protein (red). Light blue background color indicates ΔTm < 2.0 °C. (b) Graphic showing number of PKIS compounds with ΔTm > 2.0 °C (y-axis) for VRK1 (red circle) and other 67 tested kinases (x-axis, black circles). (c) Graphic showing the poor relationship between ΔTm and Gini (selectivity) coefficients for PKIS compounds interacting with VRK1. The top 3 VRK1 hits are highlighted.

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