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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:29 targets
91 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 51
pIC50 7.5 (IC50 3x10-8 M) [3H]-hypoxanthine incorporation [51]
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 52
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green incorporation (72h assay) [52]
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) [52]
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 52
pEC50 6.7 (EC50 1.8x10-7 M) [52]
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 31
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green I [31]
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 31
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I [31]
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 37
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I assay [37]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit BRD3444 PfDd2 - 8.1 pEC50 29
pEC50 8.1 (EC50 9x10-9 M) SYBR Green I assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase compound 34c [PMID: 24641010] Pf3D7 - 6.5 pEC50 54
pEC50 6.5 (EC50 3.02x10-7 M) [3H]-hypoxanthine incorporation [54]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase compound 34c [PMID: 24641010] PfNF54 - 6.6 pEC50 54
pEC50 6.6 (EC50 2.32x10-7 M) [3H]-hypoxanthine incorporation [54]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase compound 34c [PMID: 24641010] PfK1 - 6.5 pEC50 54
pEC50 6.5 (EC50 3.39x10-7 M) [3H]-hypoxanthine incorporation [54]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase compound 34c [PMID: 24641010] PfDd2 - 6.0 pEC50 54
pEC50 6.0 (EC50 9.16x10-7 M) [3H]-hypoxanthine incorporation [54]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase DDD85646 Pf - 6.6 pEC50 68
pEC50 6.6 (EC50 2.5x10-7 M) SYBR Green assay [68]
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 56
pIC50 9.1 (IC50 7x10-10 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 8.9 (IC50 1.4x10-9 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 9.2 (IC50 6x10-10 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 8.9 (IC50 1.2x10-9 M) [3H]-hypoxanthine incorporation assay [56]
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 56
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [56]
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 26
pEC50 7.5 (EC50 3x10-8 M) SYBR Green I assay [26]
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 26
pEC50 7.2 (EC50 6x10-8 M) SYBR Green I assay [26]
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 26
pEC50 7.4 (EC50 4x10-8 M) SYBR Green I assay [26]
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 26
pEC50 7.7 (EC50 2x10-8 M) SYBR Green I assay [26]
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 61
pEC50 7.7 (EC50 1.8x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.4 (EC50 3.8x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.8 (EC50 1.4x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.7 (EC50 2.2x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.5 (EC50 3.2x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.7 (EC50 1.9x10-8 M) [3H]-hypoxanthine incorporation [61]
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 61
pEC50 7.9 (EC50 1.3x10-8 M) [3H]-hypoxanthine incorporation [61]
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 11
pIC50 7.3 (IC50 5.2x10-8 M) [3H]-hypoxanthine incorporation [11]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase MMV048 PfNF54 - 7.6 pIC50 47
pIC50 7.6 (IC50 2.8x10-8 M) [3H]-hypoxanthine incorporation assay [47]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase compound 55 [PMID: 29889526] PfNF54 - 7.2 pIC50 28
pIC50 7.2 (IC50 6.3x10-8 M) [28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase compound 55 [PMID: 29889526] PfK1 - 7.0 pIC50 28
pIC50 7.0 (IC50 1.02x10-7 M) [28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase MMV024101 Pf3D7 - 6.2 pIC50 28
pIC50 6.2 (IC50 6x10-7 M) [28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase MMV024101 PfNF54 - 6.3 pIC50 28
pIC50 6.3 (IC50 5.43x10-7 M) [28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase 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 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 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 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 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 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 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 CHMFL-PI4K-127 Pf3D7 - 7.6 pEC50 35
pEC50 7.6 (EC50 2.51x10-8 M) SYBR Green I assay [35]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase CHMFL-PI4K-127 PfDd2 - 7.5 pEC50 35
pEC50 7.5 (EC50 3.03x10-8 M) SYBR Green I assay [35]
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 27
pIC50 6.5 (IC50 2.9x10-7 M) [3H]-hypoxanthine incorporation assay [27]
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 27
pIC50 6.5 (IC50 3.5x10-7 M) [3H]-hypoxanthine incorporation assay [27]
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 27
pIC50 6.4 (IC50 3.7x10-7 M) [3H]-hypoxanthine incorporation assay [27]
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 10
pIC50 7.8 (IC50 1.7x10-8 M) [3H]-hypoxanthine incorporation [10]
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 10,72
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [10]
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) [72]
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 10
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 5.2 (IC50 6.689x10-6 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 5.1 (IC50 8.231x10-6 M) [3H]-hypoxanthine incorporation [10]
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 72
pIC50 7.2 (IC50 5.8x10-8 M) [3H]-hypoxanthine incorporation assay using wild-type P. falciparum (TM4) [72]
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 72
pIC50 7.3 (IC50 5.6x10-8 M) [3H]-hypoxanthine incorporation [72]
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 72
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [72]
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 10
pIC50 8.4 (IC50 4.5x10-9 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 6.3 (IC50 4.45x10-7 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 8.8 (IC50 1.7x10-9 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 6.4 (IC50 3.657x10-7 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 6.0 (IC50 1.002x10-6 M) [3H]-hypoxanthine incorporation [10]
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 10
pIC50 5.4 (IC50 4.262x10-6 M) [3H]-hypoxanthine incorporation [10]
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 62
pIC50 7.0 (IC50 1.09x10-7 M) 72 hour growth inhibition assay [62]
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 62
pIC50 6.9 (IC50 1.2x10-7 M) 72 hour growth inhibition assay [62]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum proline--tRNA ligase halofuginone Pf3D7 - 9.1 pEC50 18
pEC50 9.1 (EC50 8.6x10-10 M) SYBR Green assay [18]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum proline--tRNA ligase halofuginone PfDd2 - 9.1 pEC50 18
pEC50 9.1 (EC50 8.1x10-10 M) SYBR Green assay [18]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonine--tRNA ligase borrelidin Pf3D7 - 8.9 – 9.0 pIC50 41
pIC50 9.0 (IC50 9.7x10-10 M) Parasite lactate dehydrogenase (pLDH ) assay following 96 hours in culture [41]
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 [41]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonine--tRNA ligase borrelidin PfK1 - 8.7 pIC50 46
pIC50 8.7 (IC50 1.9x10-9 M) Parasite lactate dehydrogenase (pLDH ) assay. [46]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum threonine--tRNA ligase borrelidin PfFCR3 - 8.7 pIC50 46
pIC50 8.7 (IC50 1.8x10-9 M) Parasite lactate dehydrogenase (pLDH ) assay [46]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysine--tRNA ligase cladosporin Pf3D7 - 7.3 pIC50 20
pIC50 7.3 (IC50 4.54x10-8 M) SYBR Green assay [20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysine--tRNA ligase cladosporin PfNF54 - 7.1 pIC50 20
pIC50 7.1 (IC50 8.79x10-8 M) SYBR Green assay [20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysine--tRNA ligase cladosporin PfK1 - 7.1 pIC50 20
pIC50 7.1 (IC50 8.01x10-8 M) SYBR Green assay [20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysine--tRNA ligase cladosporin PfD6 - 7.1 pIC50 20
pIC50 7.1 (IC50 7.21x10-8 M) SYBR Green assay [20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum lysine--tRNA ligase 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 lysine--tRNA ligase 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 lysine--tRNA ligase 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 69
pEC50 7.0 (EC50 1.1x10-7 M) [69]
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 70
pIC50 6.6 (IC50 2.5x10-7 M) SYBR green assay [70]
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 65
pIC50 7.1 (IC50 7.3x10-8 M) [3H]-hypoxanthine incorporation [65]
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 65
pIC50 6.7 (IC50 2.23x10-7 M) [3H]-hypoxanthine incorporation [65]
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 65
pIC50 5.4 (IC50 3.97x10-6 M) [3H]-hypoxanthine incorporation [65]
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 65
pIC50 8.4 (IC50 4x10-9 M) [3H]-hypoxanthine incorporation [65]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hexose transporter TCMDC-125163 Pf3D7 - 5.8 pEC50 45
pEC50 5.8 (EC50 1.4x10-6 M) SYBR Green I assay [45]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hexose transporter TCMDC-125163 PfK1 - 6.0 pEC50 45
pEC50 6.0 (EC50 9.7x10-7 M) SYBR Green I assay [45]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hexose transporter HTI-1 Pf3D7 - 6.4 pEC50 25
pEC50 6.4 (EC50 3.77x10-7 M) SYBR Green I assay [25]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum hexose transporter HTI-1 PfDd2 - 6.4 pEC50 25
pEC50 6.4 (EC50 3.98x10-7 M) SYBR Green I assay [25]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum plasmepsin X WM382 Pf3D7 - 9.2 pEC50 15
pEC50 9.2 (EC50 6x10-10 M) Results are for R-WM382 [15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum plasmepsin X WM382 PfK1 - 9.2 pEC50 15
pEC50 9.2 (EC50 6.5x10-10 M) [15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum plasmepsin X WM382 PfDd2 - 9.6 pEC50 15
pEC50 9.6 (EC50 2.6x10-10 M) [15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum plasmepsin X WM382 Pk - 9.7 pEC50 15
pEC50 9.7 (EC50 1.8x10-10 M) SYBR Green assay [15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum histone deacetylase 1 compound 1u [PMID: 30245402] Pf3D7 - 8.4 pIC50 12
pIC50 8.4 (IC50 4x10-9 M) [3H]-hypoxanthine incorporation [12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum histone deacetylase 1 compound 1u [PMID: 30245402] PfDd2 - 9.0 pIC50 12
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation [12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum histone deacetylase 1 compound 2h [PMID: 30664827] Pf3D7 - 8.3 pIC50 36
pIC50 8.3 (IC50 5.2x10-9 M) [3H]-hypoxanthine incorporation [36]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3 AN3661 Pf3D7 - 7.3 pIC50 60
pIC50 7.3 (IC50 5.2x10-8 M) [3H]-hypoxanthine incorporation [60]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3 AN3661 PfK1 - 7.7 pIC50 60
pIC50 7.7 (IC50 2x10-8 M) [3H]-hypoxanthine incorporation [60]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3 AN3661 PfDd2 - 7.4 pIC50 60
pIC50 7.4 (IC50 3.9x10-8 M) [3H]-hypoxanthine incorporation [60]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3 AN3661