Table 3. Percent inhibition values for the 4-aryl-7-azaindole PKIS2 series.
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Compound | R 1 | # kinases ≥90% Inh | Nek1 | Nek2 | Nek3 | Nek4 | Nek5 | Nek6 | Nek7 | Nek9 | Nek10 | Nek11 |
% inhibition (1 μM) | ||||||||||||
UNC5452 | 18 | 99.8 | 0 | 0 | 4 | 1 | 1 | 0 | 0 | 17 | 0 | |
UNC5023 | 42 | 62 | 0 | 14 | 0 | 44 | 4 | 0 | 22 | 69 | 24 | |
UNC5427 | 20 | 15 | 0 | 4 | 16 | 2 | 0 | 10 | 14 | 71 | 17 | |
UNC5462 | 1 | 12 | 16 | 16 | 0 | 31 | 0 | 20 | 28 | 15 | 0 | |
UNC5337 | 4 | 0 | 74 | 19 | 0 | 8 | 0 | 0 | 0 | 30 | 0 |