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Plasmepsin inhibition, antiparasitic activity, mammalian cell toxicity, and protease selectivity of Walter Reed compound WR268961
| Assay and target enzyme or cell type | IC50 (μg/ml) | Ki (μM) |
|---|---|---|
| Plasmepsin inhibition | ||
| P. falciparum | 5.8 | 6.1 |
| P. vivax | 2.5 | 1.2 |
| P. falciparum drug susceptibility | ||
| Strain W2 | 0.03 | NAa |
| Strain D6 | 0.16 | NA |
| Mammalian cell toxicity | ||
| Neuronal cells (NG-108-15) | 4 | NA |
| Macrophages (J774) | 4 | NA |
| Protease selectivity | ||
| Human cathepsin D | >450 | >280 |
NA, not applicable.
