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. 2017 Dec 8;9(1):44–66. doi: 10.1039/c7md00510e

Table 10. SAR for thienopyrimidine series for Nek4.

Inline graphic
Compound R 1 R 2 Nek4 IC50 nM Nek4 % Inh COT IC50 (nM)
Abbott Cmpd 17 graphic file with name c7md00510e-u65.jpg graphic file with name c7md00510e-u66.jpg 50 1120
Genentech Cmpd 1 graphic file with name c7md00510e-u67.jpg graphic file with name c7md00510e-u68.jpg 47.5 a 410
Genentech Cmpd 2 graphic file with name c7md00510e-u69.jpg graphic file with name c7md00510e-u70.jpg 89.9 a 150
Genentech Cmpd 32 graphic file with name c7md00510e-u71.jpg graphic file with name c7md00510e-u72.jpg 8.7 b
Abbott Cmpd 3359 graphic file with name c7md00510e-u73.jpg graphic file with name c7md00510e-u74.jpg 316
Abbott Cmpd 3357 graphic file with name c7md00510e-u75.jpg graphic file with name c7md00510e-u76.jpg 1000

a100 nM screening concentration.

b1 μM screening concentration.