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. 2018 Jan 26;8:1680. doi: 10.1038/s41598-018-19872-3

Table 1.

Kinase profiling using selected TNKS inhibitors at 10 μM. Dose response was measured for selected kinase-inhibitor pairs and inhibition-% or an IC50 is shown.

Compound CDK9 Akt p42 p38 GSK3β CK2 TNKS2
graphic file with name 41598_2018_19872_Figa_HTML.gif 34% 1% 14% 3% 57% 12% 400 nM
graphic file with name 41598_2018_19872_Figb_HTML.gif 31% 2% 3% 3% 11% 1% 15 nM
graphic file with name 41598_2018_19872_Figc_HTML.gif 16% 48% 18% 20% 4% 2% 10 nM
graphic file with name 41598_2018_19872_Figd_HTML.gif 6.2 µM 14.7 µM 660 nM
graphic file with name 41598_2018_19872_Fige_HTML.gif 16.1 µM* 13.3 µM 16 nM
graphic file with name 41598_2018_19872_Figf_HTML.gif 3.4 µM 1.6 µM 51% 45% 41% 2% 1,050 nM
graphic file with name 41598_2018_19872_Figg_HTML.gif 28.3 µM* 13.8 µM 145 nM
graphic file with name 41598_2018_19872_Figh_HTML.gif 12% 7% 2% 3% 7% 1% 5 nM
graphic file with name 41598_2018_19872_Figi_HTML.gif 9% 1% 3% 3% 3% 1% 25 nM

TNKS2 IC50 values are shown for comparison.

*The compound does not completely inhibit the enzyme at concentrations used. IC50 value extrapolated by the analysis software might be not accurately estimated.