Table 1.
Drug target | IC50 of drug (nM) | ||||||
---|---|---|---|---|---|---|---|
RWJ68198 | RWJ67657 | SD-282 | SB203580 | SB202474 | chloroquine | mefloquine | |
P. f. W2 | 380 ± 20 | 2,710 ± 190 | 8,800 ± 260 | 13,240 ± 990 | 19,530 ± 120 | 424 ± 22 | 3.59 ± 0.46 |
P. f. HB3 | 860 ± 60 | 7,630 ± 350 | 9,780 ± 790 | 12,610 ± 570 | 24,560 ± 330 | 22.0 ± 2 | 11.2 ± 0.90 |
human p38αa | 22 | 1,000 | 1.6 | 7,000 | > 10 | N/Ad | N/Ad |
T. g. TgMAPK-1b | NDc | 200 | NDc | 135 | > 10 | N/Ad | N/Ad |
IC50 data are derived as the mean and standard deviation of 3 independently derived IC50 values.
The reported IC50 value for the inhibition of purified recombinant human p38α kinase activity are taken from the following sources: RWJ68198, (Dodd et al., 2000, Rupert et al., 2003); RWJ67657, (Wadsworth et al., 1999); SB202474, (Halawani et al., 2004); SB203580, (Brumlik et al., 2004, Wadsworth et al., 1999), and SD-282 (Sweitzer et al., 2004).
The reported IC50 value for the inhibition of TgMAPK-1 autophosphorylation is taken from the following sources: SB203580, (Brumlik et al., 2004); RWJ67657 or SB202474, (Brumlik et al., unpublished observations).
ND; The IC50 value has not been determined.
N/A; Not applicable.