TABLE 4.
Selectivity of PfCDPK1 inhibitors between Plasmodium species
| Compound | IC50 (nM)a |
IC50 ratio |
|||
|---|---|---|---|---|---|
| PfCDPK1 | PbCDPK1 | PvCDPK1 | PbCDPK1/PfCDPK1 | PvCDPK1/PfCDPK1 | |
| 27 | 138 (39.5) | 479 (225.4) | 68 (16.6) | 3.5 | 0.5 |
| 28 | 40 (19.6) | 152 (43.6) | 24 (9.2) | 3.8 | 0.6 |
| 29 | 86 (37.8) | 392 (193.3) | 80 (31.6) | 4.6 | 0.9 |
| 40 | 52 (33.6) | 249 (49.4) | 48 (26.3) | 4.8 | 0.9 |
| 41 | 73 (19.2) | 206 (58.3) | 68 (15.5) | 2.8 | 0.9 |
| 42 | 109 (26.4) | 350 (56.6) | 99 (12.1) | 3.2 | 0.9 |
| 43 | 14 (3.8) | 36 (12.2) | 12 (1.8) | 2.6 | 0.8 |
| 44 | 107 (25.3) | 463 (122.9) | 59 (8.1) | 4.3 | 0.6 |
| 45 | 19 (4.1) | 58 (4.4) | 19 (2.5) | 3.0 | 1.0 |
| 46 | 13 (3.0) | 38 (2.4) | 11 (2.7) | 2.8 | 0.8 |
a
Mean IC50s were determined using ADP detection (Rh-ParM) in the absence of MTIP (n = 2) (standard deviations shown in parentheses).