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Plasmodium falciparum

Species ID:103
Name:Plasmodium falciparum
Associated with:34 targets
123 ligands
Description
P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa.

Interactions

Interactions
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Target Ligand Sp. Action Value Parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase DSM265 PfNF54 - 7.5 pIC50 74
pIC50 7.5 (IC50 3x10-8 M) [3H]-hypoxanthine incorporation [74]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM265 Pf Inhibition 7.5 pIC50 45
pIC50 7.5 (IC50 3x10-8 M) [45]
Description: Steady-state kinetic analysis.
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pf3D7 - 7.4 – 7.8 pEC50 75
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green incorporation (72h assay) [75]
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) [75]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pf Inhibition 7.3 pIC50 75
pIC50 7.3 (IC50 5.3x10-8 M) [75]
Description: Steady-state kinetic analysis of recombinant enzyme inhibition.
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 Pf3D7 - 7.8 pEC50 45
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green I [45]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 Pf Inhibition 7.7 pIC50 45
pIC50 7.7 (IC50 2x10-8 M) [45]
Description: Steady-state kinetic analysis.
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 PfDd2 - 7.8 pEC50 45
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I [45]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase BRD9185 Pf Inhibition 7.9 pIC50 55
pIC50 7.9 (IC50 1.2x10-8 M) [55]
Plasmodium falciparum dihydroorotate dehydrogenase BRD9185 PfDd2 - 7.8 pEC50 55
pEC50 7.8 (EC50 1.6x10-8 M) SYBR Green I assay [55]
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 69
pEC50 7.9 (EC50 1.2x10-8 M) SYBR Green I assay (72h) [69]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM705 Pf Inhibition 7.0 pIC50 69
pIC50 7.0 (IC50 9.5x10-8 M) [69]
Description: Steady-state kinetic analysis.
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD3444 Pf3D7 - 6.2 pEC50 42
pEC50 6.2 (EC50 6.63x10-7 M) [42]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (IV–V) gametocyte assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD3444 Pf Inhibition 7.3 pIC50 42
pIC50 7.3 (IC50 4.6x10-8 M) [42]
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 Pf3D7 - 6.8 pEC50 42
pEC50 6.8 (EC50 1.6x10-7 M) [42]
Description: Parasite late stage (IV–V) gametocyte assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD7929 Pf Inhibition 7.6 pIC50 42
pIC50 7.6 (IC50 2.3x10-8 M) [42]
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 79
pEC50 6.5 (EC50 3.02x10-7 M) [3H]-hypoxanthine incorporation [79]
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 Inhibition 8.1 pKi 79
pKi 8.1 (Ki 8x10-9 M) [79]
Description: Enzyme inhibition assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] PfNF54 - 6.6 pEC50 79
pEC50 6.6 (EC50 2.32x10-7 M) [3H]-hypoxanthine incorporation [79]
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 79
pEC50 6.5 (EC50 3.39x10-7 M) [3H]-hypoxanthine incorporation [79]
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 79
pEC50 6.0 (EC50 9.16x10-7 M) [3H]-hypoxanthine incorporation [79]
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 104
pEC50 6.6 (EC50 2.5x10-7 M) SYBR Green assay [104]
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 88
pEC50 7.5 (EC50 3.4x10-8 M) SYBR Green incorporation [88]
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 88
pEC50 7.7 (EC50 2.04x10-8 M) SYBR Green incorporation [88]
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 83
pIC50 9.1 (IC50 7x10-10 M) [3H]-hypoxanthine incorporation assay [83]
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 - - - 96
Giemsa-stained blood film counts: dose-dependent, significant inhibition of stage II gametocyte development [96]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite early stage (I–II) gametocyte assay
Oocyst count: significantly reduced count observed with the addition of cipargamin when compared to control feeds [96]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
Giemsa-stained blood film counts: dose-dependent, inhibition of stage V gametocyte development [96]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (III–V) gametocyte assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfNF54 - 9.3 pIC50 83
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [83]
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 83
pIC50 8.9 (IC50 1.4x10-9 M) [3H]-hypoxanthine incorporation assay [83]
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 83
pIC50 9.2 (IC50 6x10-10 M) [3H]-hypoxanthine incorporation assay [83]
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 83
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [83]
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 83
pIC50 8.9 (IC50 1.2x10-9 M) [3H]-hypoxanthine incorporation assay [83]
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 PfW2 - 9.1 pIC50 83
pIC50 9.1 (IC50 9x10-10 M) [3H]-hypoxanthine incorporation assay [83]
Description: Parasite growth inhibition assay
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase cipargamin PfTM90C2A - 9.3 pIC50 83
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [83]
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 PfTM91C235 - 9.1 pIC50 83
pIC50 9.1 (IC50 9x10-10 M) [3H]-hypoxanthine incorporation assay [83]
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 95
pEC50 7.7 (EC50 1.8x10-8 M) [3H]-hypoxanthine incorporation [95]
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 PfNF54 - 7.1 – 7.4 pEC50 95
pEC50 7.4 (EC50 3.9x10-8 M) inhibition of gamete formation from mature Stage V male gametocytes [95]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite dual gamete formation assay (DGFA)
pEC50 7.1 (EC50 7.4x10-8 M) inhibition of gamete formation from mature Stage V female gametocytes [95]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite dual gamete formation assay (DGFA)
Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PA21A092 PfV1/S - 7.4 pEC50 95
pEC50 7.4 (EC50 3.8x10-8 M) [3H]-hypoxanthine incorporation [95]
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 95
pEC50 7.8 (EC50 1.4x10-8 M) [3H]-hypoxanthine incorporation [95]
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 95
pEC50 7.7 (EC50 2.2x10-8 M) [3H]-hypoxanthine incorporation [95]
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 95
pEC50 7.5 (EC50 3.2x10-8 M) [3H]-hypoxanthine incorporation [95]
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 95
pEC50 7.7 (EC50 1.9x10-8 M) [3H]-hypoxanthine incorporation [95]
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 95
pEC50 7.9 (EC50 1.3x10-8 M) [3H]-hypoxanthine incorporation [95]
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 16
pIC50 7.3 (IC50 5.2x10-8 M) [3H]-hypoxanthine incorporation [16]
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 93
pIC50 6.3 (IC50 4.6x10-7 M) SYBR Green I assay [93]
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 94
pIC50 6.4 (IC50 3.8x10-7 M) SYBR Green I assay [94]
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 non-SERCA-type Ca2+ -transporting P-ATPase compound 1a [WO2021204952A1] PfNF54 - - - 24
Relative oocyst intensities, determined using transgenic reporter strain P. falciparum NF54-HGL, show that compound 1a has transmission-blocking potential [24]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
Plasmodium falciparum phosphatidylinositol 4-kinase beta MMV048 PfNF54 - 6.6 – 7.6 pIC50 70
pIC50 7.6 (IC50 2.8x10-8 M) [3H]-hypoxanthine incorporation assay [70]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
pIC50 6.8 (IC50 1.4x10-7 M) Parasite late stage (IV-V) gametocyte assay using luciferase reporter line [70]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
pIC50 6.7 (IC50 2.14x10-7 M) Parasite early stage (I-III) gametocyte assay using luciferase reporter line [70]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
pIC50 6.6 (IC50 2.85x10-7 M) Parasite late stage (IV-V) gametocyte assay: parasitic lactate dehydrogenase (pLDH) assay [70]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta MMV048 Pf - 6.9 pIC50 70
pIC50 6.9 (IC50 1.11x10-7 M) Indirect SMFA [70]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
Plasmodium falciparum phosphatidylinositol 4-kinase beta MMV048 Pf Binding 6.5 – 7.0 pKd 70
pKd 7.0 (Kd 1x10-7 M) [70]
pKd 6.5 (Kd 3x10-7 M) [70]
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 Pf - 6.9 – 7.2 pIC50 6
pIC50 7.2 (IC50 6.6x10-8 M) Parasite late stage (IV-V) gametocyte assay using luciferase reporter line [6]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
pIC50 7.1 (IC50 8x10-8 M) Reports on the functional viability of male and female mature stage V gametocytes [6]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite dual gamete formation assay (DGFA)
pIC50 7.0 (IC50 9.6x10-8 M) [6]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
pIC50 6.9 (IC50 1.34x10-7 M) Parasite early stage (I-III) gametocyte assay using luciferase reporter line [6]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability 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 52
pEC50 7.6 (EC50 2.51x10-8 M) SYBR Green I assay [52]
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 Pf Inhibition 9.1 pIC50 52
pIC50 9.1 (IC50 9x10-10 M) [52]
Plasmodium falciparum phosphatidylinositol 4-kinase beta CHMFL-PI4K-127 PfDd2 - 7.5 pEC50 52
pEC50 7.5 (EC50 3.03x10-8 M) SYBR Green I assay [52]
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 46
pEC50 9.4 (EC50 3.8x10-10 M) Viability measured using MitoProbe DiIC1(5) staining and flow cytometry [46]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta NCATS-SM3710 Pf - 8.2 pEC50 46
pEC50 8.2 (EC50 5.77x10-9 M) Viability measured using MitoProbe DiIC1(5) staining and flow cytometry [46]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (IV–V) gametocyte assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta NCATS-SM3710 Pf Inhibition 8.7 pIC50 46
pIC50 8.7 (IC50 2x10-9 M) [46]
Plasmodium falciparum phosphatidylinositol 4-kinase beta KDU691 PfNF54 - 6.7 pIC50 56
pIC50 6.7 (IC50 2.2x10-7 M) Parasite lactate dehydrogenase (pLDH) assay [56]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (III–V) gametocyte assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta KDU691 Pf - 7.5 pIC50 56
pIC50 7.5 (IC50 2.99x10-8 M) SYBR Green assay [56]
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 elongation factor 2 M5717 PfNF54 - 8.0 – 8.9 pEC50 4
pEC50 8.9 (EC50 1.2x10-9 M) Female gamete formation [4]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite gamete formation assay
pEC50 8.7 (EC50 1.8x10-9 M) Indirect SMFA [4]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
pEC50 8.7 (EC50 1.8x10-9 M) Male gamete formation [4]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite gamete formation assay
pEC50 8.0 (EC50 1x10-8 M) Direct SMFA [4]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
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 15
pIC50 7.8 (IC50 1.7x10-8 M) [3H]-hypoxanthine incorporation [15]
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 15,109
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [15]
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) [109]
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 15
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 5.2 (IC50 6.689x10-6 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 5.1 (IC50 8.231x10-6 M) [3H]-hypoxanthine incorporation [15]
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 109
pIC50 7.2 (IC50 5.8x10-8 M) [3H]-hypoxanthine incorporation assay using wild-type P. falciparum (TM4) [109]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 PfNF54 - 8.4 pIC50 76
pIC50 8.4 (IC50 4x10-9 M) Induction of male gamete activation (exflagellation) following 48 hour exposure of mature gametocytes to P218 [76]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite exflagellation assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 PfV1/S - 7.3 pIC50 109
pIC50 7.3 (IC50 5.6x10-8 M) [3H]-hypoxanthine incorporation [109]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 Pf - >7.9 pEC50 82
pEC50 >7.9 (EC50 <1.2x10-8 M) Primary human hepatocyte assay to assess inhibition of hepatic schizonts (prophylactic activity) [82]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 PfTM4 - 8.3 pIC50 109
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [109]
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 15
pIC50 8.4 (IC50 4.5x10-9 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 6.3 (IC50 4.45x10-7 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 8.8 (IC50 1.7x10-9 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 6.4 (IC50 3.657x10-7 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 6.0 (IC50 1.002x10-6 M) [3H]-hypoxanthine incorporation [15]
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 15
pIC50 5.4 (IC50 4.262x10-6 M) [3H]-hypoxanthine incorporation [15]
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 ML10 Pf3D7 Inhibition 9.8 pIC50 2
pIC50 9.8 (IC50 1.6x10-10 M) [2]
Description: microfluidic mobility shift assay
Plasmodium falciparum cGMP-dependent protein kinase MMV030084