Asexual blood stage-specific IC50 8h data in nM for some tested antimalarials | ||||||||||||||
Murithi JM, Owen ES, Istvan ES, Lee MCS, Ottilie S, Chibale K, Goldberg DE, Winzeler EA, Llinás M, Fidock DA, Vanaerschot M. Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery. Cell Chem Biol. 2019 Nov 29. pii: S2451-9456(19)30391-5. PMID: 31813848. | ||||||||||||||
Compound | Early rings | Late rings | Early trophozoites | Late trophozoites | Schizonts | Overall (72hr assay) | Peak Activity | |||||||
1.5 | 0.1 | 2.4 | 0.1 | 2.4 | 0.4 | 3.9 | 0.2 | 11.6 | 1.3 | 1.0 | 0.1 | Rings + Trophs | ||
Chloroquine | 17.8 | 5.5 | 18.6 | 2.5 | 17.4 | 3.5 | 30.1 | 6.3 | 60.3 | 13.4 | 5.9 | 0.8 | Rings + Trophs | |
Mefloquine | 258 | 106 | 147 | 74 | 28.8 | 7.0 | 29.5 | 6.9 | 138 | 39 | 9.8 | 1.0 | Trophs | |
Lumefantrine | 15.4 | 4.0 | 15.8 | 3.5 | 19.54 | 1.6 | 22.3 | 2.0 | 81.0 | 32.5 | 1.3 | 0.0 | Rings + Trophs | |
Piperaquine | 26.2 | 1.1 | 46.3 | 13.1 | 27.4 | 3.3 | 32.9 | 1.1 | 67.0 | 9.6 | 15.4 | 2.3 | Rings + Trophs | |
Ferroquine | 4.9 | 0.3 | 10.9 | 1.7 | 23.2 | 2.4 | 36.8 | 3.3 | 49.3 | 6.2 | 3.5 | 0.4 | Rings | |
Methylene blue | 3.2 | 0.3 | 13.3 | 2.7 | 5.9 | 0.4 | 8.3 | 2.0 | 64.8 | 17.8 | 1.8 | 0.1 | Rings + Trophs | |
KAI407 - shift 2 | 16263 | 904 | 14021 | 923 | 5139 | 1727 | 13386 | 354 | 46.2 | 0.6 | 11.8 | 1.0 | Schizonts | |
AN3661 | > 1.25 μM | - | > 1.25 μM | - | > 1.25 μM | - | 138 | 39 | 400 | 34 | 35.6 | 3.6 | Late Trophs | |
KAE609 | > 1.25 μM | - | > 1.25 μM | - | 3.2 | 0.6 | 1.1 | 0.2 | 1.2 | 0.1 | 0.73 | 0.05 | Trophs + Schizonts | |
WLL-vs | 23.7 | 2.6 | 29.4 | 4.4 | 57.6 | 3.1 | 47.1 | 3.1 | 50.1 | 5.7 | 7.2 | 0.8 | Rings | |
DSM265 - shift 1 | - | - | - | - | 10.2 | 2.2 | 7.7 | 0.9 | 19.2 | 2.3 | 3.8 | 0.1 | Late Trophs | |
DSM265 - shift 2 | 4821 | 1605 | 1493 | 308 | 1481 | 240 | - | - | > 25 μM | - | - | - | - | |
- | - | - | - | 0.68 | 0.06 | 3.7 | 0.2 | 7.4 | 1.3 | 1.1 | 0.1 | Late Trophs | ||
553 | 228 | 324 | 45 | 619 | 132 | - | - | > 25 μM | - | - | - | - | ||
Fosmidomycin | > 10 μM | - | > 10 μM | - | 1983 | 665 | 1993 | 117 | > 10 μM | - | 405 | 8 | Trophs | |
GNF-Pf-5660 | 119 | 30 | 238 | 57 | 108 | 6 | 79.3 | 10.8 | 290 | 50 | 4.4 | 0.2 | Rings + Trophs | |
MMV665794 | 369 | 101 | 590 | 177 | 210 | 20 | 165 | 10 | 203 | 8 | 91.3 | 5.2 | Trophs + Schizonts | |
Naphtoquine | 4.2 | 1.8 | 8.1 | 0.4 | 19.5 | 2.9 | 29.2 | 3.1 | 42.8 | 8.4 | 3.2 | 0.4 | Rings | |
MMV000442 | > 8 μΜ | - | > 8 μΜ | - | 176 | 11 | 197 | 22 | 503 | 48 | 37.2 | 3.1 | Trophs | |
MMV675939 | 1170 | 277 | 268 | 84 | 62.9 | 29.9 | 146 | 54 | 1647 | 45 | 30.8 | 4.4 | Trophs | |
MMV085071 | 893 | 78 | 492 | 122 | 61.1 | 0.1 | 81.4 | 2.8 | 254 | 47 | 105 | 11 | Trophs | |
MMV668311 | 140 | 39 | 97.7 | 4.3 | 68.9 | 11.9 | 122 | 26 | 382 | 79 | 63.5 | 1.7 | Rings + Trophs | |
MMV020746 | > 25 μM | - | > 25 μM | - | 12587 | 1681 | > 25 μM | - | > 25 μM | - | 56.8 | 6.6 | All stages > 10 μM | |
MMV667491 | 2264 | 349 | 1270 | 92 | 521 | 28 | 731 | 50 | 842 | 108 | 243 | 35 | Trophs + Schizonts | |
MMV006455 | > 12.5 μM | - | > 12.5 μM | - | 441 | 10 | 450 | 46 | 933 | 142 | 439 | 46 | Trophs | |
MMV022478 | 7628 | 202 | 4870 | 353 | 2132 | 252 | 2529 | 353 | 3370 | 269 | 11.1 | 0.8 | Trophs + Schizonts | |
MMV007181 | > 25 μM | - | > 25 μM | - | 253 | 27 | 274 | 16 | 570 | 107 | 84.9 | 8.9 | Trophs | |
MMV665971 | > 25 μM | - | > 25 μM | - | 496 | 51 | 485 | 26 | 523 | 29 | 185 | 9 | Trophs + Schizonts | |
MMV665939 | 17011 | 2420 | 22853 | 5330 | 13476 | 4752 | 39017 | 13066 | 54384 | 14265 | 478 | 49 | All stages > 10 μM | |
MMV019017 | 8418 | 1862 | 8663 | 2298 | 1338 | 133 | 1708 | 116 | 3060 | 229 | 306 | 12 | Trophs + Schizonts | |
MMV000248 | n.d. | n.d. | 6744 | - | 411 | - | 376 | - | 754 | - | 103 | 14 | Trophs | |
MMV021735 | > 25 μM | - | > 25 μM | - | 5422 | 1392 | 234 | 12 | 5281 | 622 | 232 | 11 | Late Trophs | |
MMV022224 | 838 | 123 | 845 | 152 | 542 | 39 | 752 | 58 | 2486 | 472 | 199 | 31 | Rings + Trophs | |
MMV027496 | 2760 | 529 | 878 | 130 | 168 | 26 | 199 | 9 | 4339 | 545 | 89.7 | 7.9 | Trophs | |
MMV027496 | 755 | 159 | 788 | 221 | 81.4 | 1.6 | 110 | 20 | 349 | 66 | 33.3 | 1.8 | Trophs | |
MMV030666 | 10264 | 3053 | 11440 | 861 | 5124 | 506 | 858 | 29 | 4191 | 307 | 462 | 18 | Late Trophs | |
MMV000787 | 5737 | 1215 | 7870 | 731 | 3312 | 629 | 1354 | 57 | 5912 | 617 | 1960 | 83 | Late Trophs | |
Shift 1 and shift 2 indicate the two half-maximal inhibitory concentrations for biphasic dose response curves. SEM: standard error of the mean; n: number of biological repeats; - : no data; IC508h: IC50 based on 8-h exposure; IC5072h: IC50 based on 72-h exposure. |