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
Dihydroartemisinin 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 - - - -
Atovaquone - shift 1 - - - - 0.68 0.06 3.7 0.2 7.4 1.3 1.1 0.1 Late Trophs
Atovaquone - shift 2 553 228 324 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.
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