TABLE 1.
MMV1557817 effectiveness against drug-resistant P. falciparum strainsa
| Parasite strain | EC50 nM (mean)b | Fold shift EC50 relative to | Altered genes | |
|---|---|---|---|---|
| NF54 | Dd2 | |||
| NF54 | 22 | 1.0 | Sensitive strain | |
| K1 | 26 | 1.2 | Pfcrt, Pfmdr1, Pfdhfr, Pfdhps | |
| 7G8 | 28 | 1.3 | Pfcrt, Pfmdr1, Pfdhfr, Pfdhps | |
| TM90C2B | 21 | 1.0 | Pfcrt, Pfmdr1, Pfdhfr, Pfdhps, PfcytbQ0 | |
| Cam3.1 (MRA1240) | 23 | 1.1 | Pfcrt, Pfmdr1, Pfdhfr, Pfdhps, Pfkelch13 | |
| Dd2 | 23 | 1.1 | 1.0 | Pfcrt, Pfmdr1, Pfdhfr, Pfdhps |
| Dd2 DDD107498 | 24 | 1.0 | Dd2 + Pfeef2 | |
| Dd2 MMV390048 | 19 | 0.8 | Dd2 + Pfpi4k | |
| Dd2 DSM265 | 21 | 0.9 | Dd2 + Pfdhodh | |
| Dd2 GNF156 | 22 | 1.0 | Dd2 + Pfcarl | |
| Dd2 ELQ300 | 22 | 1.0 | Dd2 + PfcytB | |
a
Seventy-two-hour [3H]hypoxanthine incorporation assay.
b
Mean values from two independent biological replicates.