Table 2. IC50 values for benzothiazole inhibitors showing activity at 50 μM.
IC50 values were determined using the SPA as described for PfNMT and HsNMT1. Compounds previously evaluated as inhibitors of TbNMT and LmNMT (denoted with *; [27]) were investigated together with benzothiazole-based inhibitors (structures 1–7 in Figure 3) that show inhibitory activity at 50 μM.
| IC50 value determined in SPA (μM) | ||
|---|---|---|
| Inhibitor | PfNMT | HsNMT |
| CP-005240 (*) | 0.36±0.04 | 1.8±0.3 |
| CP-014553 (*) | 0.28±0.12 | 1.6±0.5 |
| CP-144568 (*) | 300±78 | >1000 |
| UK-370485 (*) | 232±46 | >1000 |
| UK-145974 (*) | >1000 | >1000 |
| UK-370309 (4) | 17±1 | 331±29 |
| UK-370509 (1) | 30±3 | 286±93 |
| UK-370624 (5) | 53±5 | 656±210 |
| UK-370709 (6) | 111±7 | 711±133 |
| UK-370710 (2) | 115±9 | 28±9 |
| UK-362799 (3) | 68±4 | 309±58 |
| UK-370713 (7) | 37±4 | 329±84 |