TABLE 1.
Data for CDPK1 inhibitors
| Compound no. | Compound | clogPa | CpCDPK1 IC50 (nM) | C. parvum EC50 (μM) | Src IC50 (μM) | CRL-8155 EC50 (μM) | hERG EC50 (μM) |
|---|---|---|---|---|---|---|---|
| 2 | 1517 | 2.61 | 1.4b | 0.65 | >30b | >30b | >30 |
| 4 | 1597 | 3.20 | 2.3 | 0.41 | >10b | >40b | >30 |
| 5 | 1473 | 3.44 | 3.6b | 1.00 | 7.3b | >30b | NDc |
| 6 | 1598 | 2.33 | 5.1 | 2.16 | >10b | >40b | ND |
| 7 | 1635 | 2.93 | 3.7 | 3.35 | 10b | >40b | ND |
| 8 | 1779 | 3.16 | 0.03 | 1.03 | >10 | >80 | ND |
| 9 | 1571 | 3.35 | 4.3 | 14.85 | >10b | >40b | 30.0 |
| 10 | 1633 | 3.95 | 2.5 | 6.66 | >10b | >40b | 14.1 |
| 11 | 1776 | 4.18 | 0.3 | 3.29 | >10 | 30 | ND |
| 12 | 1586 | 2.71 | 4.9 | 0.58 | 4.75b | >40b | 22.8 |
| 13 | 1643 | 3.31 | 2.5 | 0.41 | >10b | >40b | >30 |
| 14 | 1673 | 3.55 | 4.3 | 0.52 | >10 | >40 | 27.0 |
| 15 | 1566 | 3.13 | 3.1 | >20 | >10b | >40b | ND |
| 16 | 1608 | 1.34 | 5.5 | 0.71 | 3.5 | 40 | >30 |
| 17 | 1656 | 3.61 | 2.7 | 1.00 | >10 | >40 | 11.9 |
| 18 | Paromomycin | >2,000 | 96.6 | >10 | >40 | ND |