Table 3.
PLK1 Inhibitors Show Pf NEK3 Inhibition In Vitroa
compound | % activity remaining at 2.5 μM in plasmodial kinases | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
ARK1 | ARK3 | CDPK2 | CDPK5 | GSK3 | NEK1 | NEK3 | PK5 | PK6 | PK9 | PKB | |
1 | 100.0 | 100.0 | 80.6 | 100.0 | 99.4 | 94.5 | 4.7 (86 ± 11) | 100.0 | 94.6 | 97.2 | 100.0 |
2 | 53.4 | 73.5 | 100.0 | 100.0 | 100.0 | 93.3 | 39.6 (1480 ± 150) | 100.0 | 94.8 | 100.0 | 64.2 |
11 | 100.0 | 83.6 | 100.0 | 100.0 | 100.0 | 93.8 | 11.1 (130 ± 20) | 100.0 | 67.3 | 100.0 | 49.3 |
12 | 99.5 | 96.2 | 100.0 | 100.0 | 100.0 | 100.0 | 9.7 (19 ± 30) | 100.0 | 100.0 | 100.0 | 100.0 |
18 | 73.9 | 84.6 | 24.0 (390 ± 50) | 88.1 | 100.0 | 96.4 | 15.4 (630 ± 120) | 100.0 | 78.9 | 78.7 | 12.3 (250 ± 60) |
19 | 77.9 | 83.6 | 36.1 (780 ± 90) | 100.0 | 100.0 | 90.1 | 18.5 (1820 ± 210) | 100.0 | 91.0 | 85.7 | 14.8 (790 ± 140) |
Values are % activity remaining.
Values in parentheses are IC50 values in nM ± SD.