Table 3. Activity values/properties of NMT inhibitors identified in Pfizer high-throughput screen.1 , 2 .
| IC50 L.don. NMT | EC50 extracellular L. donovani amastigotes | LD50 bone marrow derived macrophages | pKa | cLogP | Hydrogen bond donors | |
| IMP-0000083 (analogue of PF-00349412) | 281 nM | 24 µM | >45 µM | 8.4 | 2.6 | 0 |
| IMP-0000556 (PF-03393842) | 316 nM | no activity up to 30 µM | >45 µM | 10.0 | 3.1 | 2 |
| IMP-0000195 (PF-03402623) | 77 nM | 12 µM | 12 µM | 8.9 | 2.9 | 2 |
| IMP-0000197 (PF-00075634) | 914 nM | 16 µM | 50 µM | 9.8 | 4.5 | 1 |
1
Ref 35.
2
structures shown in Fig. 4B.