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

Table 12. Imidazotriazine structures and percent inhibition values.

Inline graphic
Compound R 1 # kinases ≥90% Inh Nek1 Nek2 Nek3 Nek4 Nek5 Nek6 Nek7 Nek9 Nek10 Nek11
% Inhibition (a. 1 μM b. 100 nM)
GW7331 a graphic file with name c7md00510e-u89.jpg 0 a. 22% a. 38% a. 9% a. 10% a. 86%
b. 5% b. 8% b. 4% b. 6% b. 55%
GW1893 a graphic file with name c7md00510e-u90.jpg 0 a. 11% a. 32% a. 81% a. 2% a. –1%
b. 3% b. 7% b. 29% b. 4% b. 3%
UNC5391 b graphic file with name c7md00510e-u91.jpg 0 a. 16% a. 70% a. 89% a. 41% a. 99% a. 70% a. 70% a. 70% a. 0% a. 86%
b. — b. — b. — b. — b. — b. — b. — b. — b. — b. —

a PKIS – Nanosyn screening data (Ellkins et al., 2016).

b PKIS2 – DiscoverX screening data (Drewry et al., 2017).