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Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)

Stage ID:3
Name:Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Associated with:33 targets
118 ligands
Description
The collective lifecycle stage that occurs as a result of asexual replication in erythrocytes of the host organism and can include:
  • erythrocytic merozoite, non-motile but recognises specific proteins on the surface of the erythrocyte and has an apical complex that facilitates entry into the host cell. This form of the parasite is also found in host hepatocytes (see hepatic merozoites).
  • trophozoite, the intracellular trophic form that develops from the merozoite. The young trophozoite has a distinctive 'ring' morphology in Geimsa-stained blood smears but this disappears as the parasite grows in size. During the trophic period the parasite ingests the host cell cytoplasm and breaks down the haemoglobin, producing non-toxic hemozoin as a by-product. After feeding and growth is complete the trophozoite undergoes asexual reproduction (schizony) and develops into a schizont.
  • erythrocytic schizont, a multinucleate form of the parasite that develops in erythrocytes from the trophozoite by schizogony with incomplete cytokineses. This developmental form is also found in host hepatocytes (see hepatic schizont).
Completion of cytokinesis produces several thousand merozoites from a single schizont, leading to rupture of the infected erythrocyte and release of merozoites into the bloodstream. These merozoites invade new erythrocytes and initiate either another cycle of schizogony or, under certain conditions, a small percentage of merozoites commit to sexual reproduction instead (see Plasmodium sexual blood stage).
It is the repeated cycles of schizogony in erythrocytes that leads to clinical symptoms: the simultaneous rupture of infected erythrocytes and the associated release of antigens and waste products accounts for the intermittent bouts of fever associated with malaria. As a result, almost all available antimalarial therapies target the asexual blood stage.

Interactions

Interactions
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Target Ligand Sp. Action Value Parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase DSM265 PfNF54 - 7.5 pIC50 71
pIC50 7.5 (IC50 3x10-8 M) [3H]-hypoxanthine incorporation [71]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pf3D7 - 7.4 – 7.8 pEC50 72
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green incorporation (72h assay) [72]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
pEC50 7.4 (EC50 4.3x10-8 M) SYBR Green incorporation (48h assay) [72]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pv - 6.7 pEC50 72
pEC50 6.7 (EC50 1.8x10-7 M) [72]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Blood-stage: schizont maturation assay using P. vivax field isolates.
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 Pf3D7 - 7.8 pEC50 44
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green I [44]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 PfDd2 - 7.8 pEC50 44
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I [44]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase BRD9185 PfDd2 - 7.8 pEC50 53
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I assay [53]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM705 Pf3D7 - 7.9 pEC50 66
pEC50 7.9 (EC50 1.2x10-8 M) SYBR Green I assay (72h) [66]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD3444 PfDd2 - 8.1 pEC50 42
pEC50 8.1 (EC50 9x10-9 M) SYBR Green I assay [42]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD7929 PfDd2 - 8.1 pEC50 42
pEC50 8.1 (EC50 9x10-9 M) SYBR Green I assay [42]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] Pf3D7 - 6.5 pEC50 75
pEC50 6.5 (EC50 3.02x10-7 M) [3H]-hypoxanthine incorporation [75]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] PfNF54 - 6.6 pEC50 75
pEC50 6.6 (EC50 2.32x10-7 M) [3H]-hypoxanthine incorporation [75]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] PfK1 - 6.5 pEC50 75
pEC50 6.5 (EC50 3.39x10-7 M) [3H]-hypoxanthine incorporation [75]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] PfDd2 - 6.0 pEC50 75
pEC50 6.0 (EC50 9.16x10-7 M) [3H]-hypoxanthine incorporation [75]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase DDD85646 Pf - 6.6 pEC50 95
pEC50 6.6 (EC50 2.5x10-7 M) SYBR Green assay [95]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase IMP-1002 Pf3D7 - 7.5 pEC50 81
pEC50 7.5 (EC50 3.4x10-8 M) SYBR Green incorporation [81]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum N-myristoyltransferase IMP-1002 PfDd2 - 7.7 pEC50 81
pEC50 7.7 (EC50 2.04x10-8 M) SYBR Green incorporation [81]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin Pf3D7 - 9.1 pIC50 77
pIC50 9.1 (IC50 7x10-10 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfNF54 - 9.3 pIC50 77
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfV1/S - 8.9 pIC50 77
pIC50 8.9 (IC50 1.4x10-9 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfK1 - 9.2 pIC50 77
pIC50 9.2 (IC50 6x10-10 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfD6 - 9.0 pIC50 77
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin Pf7G8 - 8.9 pIC50 77
pIC50 8.9 (IC50 1.2x10-9 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfTM90C2A - 9.3 pIC50 77
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [77]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase (+)-SJ733 Pf3D7 - 7.5 pEC50 38
pEC50 7.5 (EC50 3x10-8 M) SYBR Green I assay [38]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase (+)-SJ733 PfV1/S - 7.2 pEC50 38
pEC50 7.2 (EC50 6x10-8 M) SYBR Green I assay [38]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase (+)-SJ733 PfK1 - 7.4 pEC50 38
pEC50 7.4 (EC50 4x10-8 M) SYBR Green I assay [38]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase (+)-SJ733 PfDd2 - 7.7 pEC50 38
pEC50 7.7 (EC50 2x10-8 M) SYBR Green I assay [38]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 Pf3D7 - 7.7 pEC50 87
pEC50 7.7 (EC50 1.8x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfV1/S - 7.4 pEC50 87
pEC50 7.4 (EC50 3.8x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfTM90C2A - 7.8 pEC50 87
pEC50 7.8 (EC50 1.4x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfDd2 - 7.7 pEC50 87
pEC50 7.7 (EC50 2.2x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfHB3 - 7.5 pEC50 87
pEC50 7.5 (EC50 3.2x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfFCR3 - 7.7 pEC50 87
pEC50 7.7 (EC50 1.9x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfTM90C2B - 7.9 pEC50 87
pEC50 7.9 (EC50 1.3x10-8 M) [3H]-hypoxanthine incorporation [87]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase GSK030 Pf - 7.3 pIC50 17
pIC50 7.3 (IC50 5.2x10-8 M) [3H]-hypoxanthine incorporation [17]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase MMV1803022 Pf3D7 - 6.3 pIC50 85
pIC50 6.3 (IC50 4.6x10-7 M) SYBR Green I assay [85]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase MMV897698 Pf3D7 - 6.4 pIC50 86
pIC50 6.4 (IC50 3.8x10-7 M) SYBR Green I assay [86]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase compound 1a [WO2021204952A1] Pf3D7 - 7.7 pEC50 24
pEC50 7.7 (EC50 1.9x10-8 M) SYBR Green assay [24]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta MMV048 PfNF54 - 7.6 pIC50 67
pIC50 7.6 (IC50 2.8x10-8 M) [3H]-hypoxanthine incorporation assay [67]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta compound 55 [PMID: 29889526] PfNF54 - 7.2 pIC50 41
pIC50 7.2 (IC50 6.3x10-8 M) Parasite lactate dehydrogenase (pLDH ) assay [41]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta compound 55 [PMID: 29889526] PfK1 - 7.0 pIC50 41
pIC50 7.0 (IC50 1.02x10-7 M) Parasite lactate dehydrogenase (pLDH ) assay [41]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta MMV024101 PfNF54 - 6.3 pIC50 41
pIC50 6.3 (IC50 5.43x10-7 M) Parasite lactate dehydrogenase (pLDH ) assay [41]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfNF54 - 8.3 pIC50 6
pIC50 8.3 (IC50 5.4x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfV1/S - 8.4 pIC50 6
pIC50 8.4 (IC50 4.2x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfK1 - 8.3 pIC50 6
pIC50 8.3 (IC50 4.7x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfD6 - 8.3 pIC50 6
pIC50 8.3 (IC50 5.2x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 Pf7G8 - 8.4 pIC50 6
pIC50 8.4 (IC50 4.1x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfDd2 - 8.2 pIC50 6
pIC50 8.2 (IC50 5.7x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 PfHB3 - 8.4 pIC50 6
pIC50 8.4 (IC50 3.7x10-9 M) [3H]-hypoxanthine incorporation [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta CHMFL-PI4K-127 Pf3D7 - 7.6 pEC50 50
pEC50 7.6 (EC50 2.51x10-8 M) SYBR Green I assay [50]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta CHMFL-PI4K-127 PfDd2 - 7.5 pEC50 50
pEC50 7.5 (EC50 3.03x10-8 M) SYBR Green I assay [50]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta NCATS-SM3710 PfNF54 - 9.4 pEC50 45
pEC50 9.4 (EC50 3.8x10-10 M) Viability measured using MitoProbe DiIC1(5) staining and flow cytometry [45]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta KDU691 Pf - 7.5 pIC50 54
pIC50 7.5 (IC50 2.99x10-8 M) SYBR Green assay [54]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum elongation factor 2 M5717 Pf3D7 - 9.0 pEC50 4
pEC50 9.0 (EC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase fosmidomycin PfDd2 - 6.5 pIC50 39
pIC50 6.5 (IC50 2.9x10-7 M) [3H]-hypoxanthine incorporation assay [39]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase fosmidomycin PfHB3 - 6.5 pIC50 39
pIC50 6.5 (IC50 3.5x10-7 M) [3H]-hypoxanthine incorporation assay [39]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase fosmidomycin PfA2 - 6.4 pIC50 39
pIC50 6.4 (IC50 3.7x10-7 M) [3H]-hypoxanthine incorporation assay [39]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfNF54 - 7.8 pIC50 16
pIC50 7.8 (IC50 1.7x10-8 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfV1/S - <4.0 – 5.0 pIC50 16,99
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
pIC50 <4.0 (IC50 >1x10-4 M) [3H]-hypoxanthine incorporation assay using quadruple mutant P. falciparum (V1/S) [99]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfK1 - <5.0 pIC50 16
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfD6 - 8.3 pIC50 16
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine Pf7G8 - 5.2 pIC50 16
pIC50 5.2 (IC50 6.689x10-6 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfW2 - <5.0 pIC50 16
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfTM90C2A - 5.1 pIC50 16
pIC50 5.1 (IC50 8.231x10-6 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase pyrimethamine PfTM4 - 7.2 pIC50 99
pIC50 7.2 (IC50 5.8x10-8 M) [3H]-hypoxanthine incorporation assay using wild-type P. falciparum (TM4) [99]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 PfV1/S - 7.3 pIC50 99
pIC50 7.3 (IC50 5.6x10-8 M) [3H]-hypoxanthine incorporation [99]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 PfTM4 - 8.3 pIC50 99
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [99]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfNF54 - 8.4 pIC50 16
pIC50 8.4 (IC50 4.5x10-9 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfV1/S - <5.0 pIC50 16
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfK1 - 6.3 pIC50 16
pIC50 6.3 (IC50 4.45x10-7 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfD6 - 8.8 pIC50 16
pIC50 8.8 (IC50 1.7x10-9 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil Pf7G8 - 6.4 pIC50 16
pIC50 6.4 (IC50 3.657x10-7 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfW2 - 6.0 pIC50 16
pIC50 6.0 (IC50 1.002x10-6 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase cycloguanil PfTM90C2A - 5.4 pIC50 16
pIC50 5.4 (IC50 4.262x10-6 M) [3H]-hypoxanthine incorporation [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cGMP-dependent protein kinase ML10 Pf3D7 - 8.7 pEC50 2
pEC50 8.7 (EC50 2.1x10-9 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cGMP-dependent protein kinase MMV030084 Pf3D7 - 7.0 pIC50 88
pIC50 7.0 (IC50 1.09x10-7 M) 72 hour growth inhibition assay [88]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cGMP-dependent protein kinase MMV030084 PfDd2 - 6.9 pIC50 88
pIC50 6.9 (IC50 1.2x10-7 M) 72 hour growth inhibition assay [88]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase halofuginone Pf3D7 - 9.1 pEC50 27
pEC50 9.1 (EC50 8.6x10-10 M) SYBR Green assay [27]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase halofuginone PfDd2 - 9.1 pEC50 27
pEC50 9.1 (EC50 8.1x10-10 M) SYBR Green assay [27]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] Pf3D7 - 8.0 pIC50 63
pIC50 8.0 (IC50 1x10-8 M) DAPI incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] PfNF54 - 7.7 pIC50 63
pIC50 7.7 (IC50 1.8x10-8 M) [3H]-hypoxanthine incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] PfK1 - 7.7 pIC50 63
pIC50 7.7 (IC50 2x10-8 M) [3H]-hypoxanthine incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] Pf7G8 - 7.7 pIC50 63
pIC50 7.7 (IC50 1.8x10-8 M) [3H]-hypoxanthine incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] PfDd2 - 7.6 pIC50 63
pIC50 7.6 (IC50 2.4x10-8 M) [3H]-hypoxanthine incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum prolyl-tRNA synthetase compound 1 [PMID: 33929818] PfTM90C2B - 7.8 pIC50 63
pIC50 7.8 (IC50 1.7x10-8 M) [3H]-hypoxanthine incorporation assay (72h) [63]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonyl-tRNA synthetase borrelidin Pf3D7 - 8.9 – 9.0 pIC50 59
pIC50 9.0 (IC50 9.7x10-10 M) Parasite lactate dehydrogenase (pLDH ) assay following 96 hours in culture [59]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
pIC50 8.9 (IC50 1.24x10-9 M) Parasite lactate dehydrogenase (pLDH ) assay following 48 hours in culture [59]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonyl-tRNA synthetase borrelidin PfK1 - 8.7 pIC50 65
pIC50 8.7 (IC50 1.9x10-9 M) Parasite lactate dehydrogenase (pLDH ) assay. [65]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonyl-tRNA synthetase borrelidin PfFCR3 - 8.7 pIC50 65
pIC50 8.7 (IC50 1.8x10-9 M) Parasite lactate dehydrogenase (pLDH ) assay [65]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase cladosporin Pf3D7 - 7.3 pIC50 29
pIC50 7.3 (IC50 4.54x10-8 M) SYBR Green assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase cladosporin PfNF54 - 7.1 pIC50 29
pIC50 7.1 (IC50 8.79x10-8 M) SYBR Green assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase cladosporin PfK1 - 7.1 pIC50 29
pIC50 7.1 (IC50 8.01x10-8 M) SYBR Green assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase cladosporin PfD6 - 7.1 pIC50 29
pIC50 7.1 (IC50 7.21x10-8 M) SYBR Green assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase compound 5 [PMID: 30894487] Pf3D7 - 6.6 pEC50 3
pEC50 6.6 (EC50 2.7x10-7 M) SYBRgreen I [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase compound 5 [PMID: 30894487] PfNF54 - 6.4 pEC50 3
pEC50 6.4 (EC50 3.9x10-7 M) [3H]-hypoxanthine incorporation [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysyl-tRNA synthetase compound 5 [PMID: 30894487] PfK1 - 6.3 pEC50 3
pEC50 6.3 (EC50 5.1x10-7 M) [3H]-hypoxanthine incorporation [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase MMV008138 PfW2 - 7.0 pEC50 96
pEC50 7.0 (EC50 1.1x10-7 M) [96]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase MMV008138 PfDd2 - 6.6 pIC50 97
pIC50 6.6 (IC50 2.5x10-7 M) SYBR green assay [97]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase sulfadoxine Pf3D7 - 7.1 pIC50 92
pIC50 7.1 (IC50 7.3x10-8 M) [3H]-hypoxanthine incorporation [92]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase sulfadoxine PfK1 - 6.7 pIC50 92
pIC50 6.7 (IC50 2.23x10-7 M) [3H]-hypoxanthine incorporation [92]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase sulfadoxine PfDd2 - 5.4 pIC50 92
pIC50 5.4 (IC50 3.97x10-6 M) [3H]-hypoxanthine incorporation [92]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase sulfadoxine PfHB3 - 8.4 pIC50 92
pIC50 8.4