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Plasmodium falciparum

Species ID:103
Name:Plasmodium falciparum
Associated with:19 targets
51 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 Affinity Parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pf3D7 - 7.4 – 7.8 pEC50 27
pEC50 7.8 (EC50 1.4x10-8 M) SYBR Green incorporation (72h assay) [27]
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) [27]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum dihydroorotate dehydrogenase DSM265 PfNF54 - 7.5 pIC50 26
pIC50 7.5 (IC50 3x10-8 M) [3H]-hypoxanthine incorporation [26]
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 27
pIC50 7.3 (IC50 5.3x10-8 M) [27]
Description: Steady-state kinetic analysis of recombinant enzyme inhibition.
Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit BRD3444 Pf3D7 Inhibition 7.3 pIC50 17
pIC50 7.3 (IC50 4.6x10-8 M) [17]
Plasmodium falciparum N-Myristoyltransferase compound 34c [PMID: 24641010] Pf3D7 - 6.5 pEC50 28
pEC50 6.5 (EC50 3.02x10-7 M) [3H]-hypoxanthine incorporation [28]
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 28
pKi 8.1 (Ki 8x10-9 M) [28]
Description: Enzyme inhibition assay
Plasmodium falciparum N-Myristoyltransferase compound 34c [PMID: 24641010] PfNF54 - 6.6 pEC50 28
pEC50 6.6 (EC50 2.32x10-7 M) [3H]-hypoxanthine incorporation [28]
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 28
pEC50 6.5 (EC50 3.39x10-7 M) [3H]-hypoxanthine incorporation [28]
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 28
pEC50 6.0 (EC50 9.16x10-7 M) [3H]-hypoxanthine incorporation [28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 (+)-SJ733 Pf3D7 - 7.5 pEC50 14
pEC50 7.5 (EC50 3x10-8 M) SYBR Green I assay [14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin Pf3D7 - 9.1 pIC50 29
pIC50 9.1 (IC50 7x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfNF54 - - - 33
Giemsa-stained blood film counts: dose-dependent, significant inhibition of stage II gametocyte development [33]
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 [33]
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 [33]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (III–V) gametocyte assay
Plasmodium falciparum ATPase4 cipargamin PfNF54 - 9.3 pIC50 29
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 (+)-SJ733 PfV1/S - 7.2 pEC50 14
pEC50 7.2 (EC50 6x10-8 M) SYBR Green I assay [14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfV1/S - 8.9 pIC50 29
pIC50 8.9 (IC50 1.4x10-9 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 (+)-SJ733 PfK1 - 7.4 pEC50 14
pEC50 7.4 (EC50 4x10-8 M) SYBR Green I assay [14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfK1 - 9.2 pIC50 29
pIC50 9.2 (IC50 6x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfD6 - 9.0 pIC50 29
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin Pf7G8 - 8.9 pIC50 29
pIC50 8.9 (IC50 1.2x10-9 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfW2 - 9.1 pIC50 29
pIC50 9.1 (IC50 9x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfTM90C2A - 9.3 pIC50 29
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 cipargamin PfTM91C235 - 9.1 pIC50 29
pIC50 9.1 (IC50 9x10-10 M) [3H]-hypoxanthine incorporation assay [29]
Description: Parasite growth inhibition assay
Plasmodium falciparum ATPase4 (+)-SJ733 PfDd2 - 7.7 pEC50 14
pEC50 7.7 (EC50 2x10-8 M) SYBR Green I assay [14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase MMV024101 Pf3D7 - 6.2 pIC50 16
pIC50 6.2 (IC50 6x10-7 M) [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase MMV024101 PfNF54 - 6.3 pIC50 16
pIC50 6.3 (IC50 5.43x10-7 M) [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase compound 55 [PMID: 29889526] PfNF54 - 7.2 pIC50 16
pIC50 7.2 (IC50 6.3x10-8 M) [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase MMV048 PfNF54 - 6.8 – 7.6 pIC50 24
pIC50 7.6 (IC50 2.8x10-8 M) [3H]-hypoxanthine incorporation assay [24]
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 [24]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
Plasmodium falciparum phosphatidylinositol 4-kinase UCT943 PfNF54 - 8.3 pIC50 4
pIC50 8.3 (IC50 5.4x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase MMV048 PfNF54 - 6.6 – 6.7 pIC50 24
pIC50 6.7 (IC50 2.14x10-7 M) Parasite early stage (I-III) gametocyte assay using luciferase reporter line [24]
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 [24]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
Plasmodium falciparum phosphatidylinositol 4-kinase UCT943 PfV1/S - 8.4 pIC50 4
pIC50 8.4 (IC50 4.2x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum phosphatidylinositol 4-kinase UCT943 Pf - 6.9 – 7.2 pIC50 4
pIC50 7.2 (IC50 6.6x10-8 M) Parasite late stage (IV-V) gametocyte assay using luciferase reporter line [4]
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 [4]
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)
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 [4]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
Plasmodium falciparum phosphatidylinositol 4-kinase MMV048 Pf - 6.9 pIC50 24
pIC50 6.9 (IC50 1.11x10-7 M) Indirect SMFA [24]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
Plasmodium falciparum phosphatidylinositol 4-kinase MMV048 Pf Binding 6.5 – 7.0 pKd 24
pKd 7.0 (Kd 1x10-7 M) [24]
pKd 6.5 (Kd 3x10-7 M) [24]
Plasmodium falciparum phosphatidylinositol 4-kinase compound 55 [PMID: 29889526] PfK1 - 7.0 pIC50 16
pIC50 7.0 (IC50 1.02x10-7 M) [16]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Plasmodium falciparum phosphatidylinositol 4-kinase UCT943 PfK1 - 8.3 pIC50 4
pIC50 8.3 (IC50 4.7x10-9 M) [3H]-hypoxanthine incorporation [4]
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 4
pIC50 8.3 (IC50 5.2x10-9 M) [3H]-hypoxanthine incorporation [4]
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 4
pIC50 8.4 (IC50 4.1x10-9 M) [3H]-hypoxanthine incorporation [4]
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 4
pIC50 8.2 (IC50 5.7x10-9 M) [3H]-hypoxanthine incorporation [4]
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 4
pIC50 8.4 (IC50 3.7x10-9 M) [3H]-hypoxanthine incorporation [4]
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 2
pEC50 9.0 (EC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [2]
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 2
pEC50 8.9 (EC50 1.2x10-9 M) Female gamete formation [2]
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) Male gamete formation [2]
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 [2]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
pEC50 8.0 (EC50 1x10-8 M) Direct SMFA [2]
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 15
pIC50 6.5 (IC50 2.9x10-7 M) [3H]-hypoxanthine incorporation assay [15]
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 15
pIC50 6.5 (IC50 3.5x10-7 M) [3H]-hypoxanthine incorporation assay [15]
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 15
pIC50 6.4 (IC50 3.7x10-7 M) [3H]-hypoxanthine incorporation assay [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 PfNF54 - 8.4 pIC50 7
pIC50 8.4 (IC50 4.5x10-9 M) [3H]-hypoxanthine incorporation [7]
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 7
pIC50 <5.0 (IC50 >1x10-5 M) [3H]-hypoxanthine incorporation [7]
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 39
pIC50 7.3 (IC50 5.6x10-8 M) [3H]-hypoxanthine incorporation [39]
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 7
pIC50 6.3 (IC50 4.45x10-7 M) [3H]-hypoxanthine incorporation [7]
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 7
pIC50 8.8 (IC50 1.7x10-9 M) [3H]-hypoxanthine incorporation [7]
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 7
pIC50 6.4 (IC50 3.657x10-7 M) [3H]-hypoxanthine incorporation [7]
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 7
pIC50 6.0 (IC50 1.002x10-6 M) [3H]-hypoxanthine incorporation [7]
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 7
pIC50 5.4 (IC50 4.262x10-6 M) [3H]-hypoxanthine incorporation [7]
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 39
pIC50 8.3 (IC50 4.6x10-9 M) [3H]-hypoxanthine incorporation [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 PfTM4 - 7.2 pIC50 39
pIC50 7.2 (IC50 5.8x10-8 M) [3H]-hypoxanthine incorporation assay wild-type P. falciparum (TM4) [39]
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 1
pEC50 8.7 (EC50 2.1x10-9 M) [3H]-hypoxanthine incorporation [1]
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 1
pIC50 9.8 (IC50 1.6x10-10 M) [1]
Description: microfluidic mobility shift assay
Plasmodium falciparum proline--tRNA ligase halofuginone Pf3D7 - 9.1 pEC50 12
pEC50 9.1 (EC50 8.6x10-10 M) SYBR Green assay [12]
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 12
pEC50 9.1 (EC50 8.1x10-10 M) SYBR Green assay [12]
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 13
pIC50 7.3 (IC50 4.54x10-8 M) SYBR Green assay [13]
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 13
pIC50 7.1 (IC50 8.79x10-8 M) SYBR Green assay [13]
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 13
pIC50 7.1 (IC50 8.01x10-8 M) SYBR Green assay [13]
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 13
pIC50 7.1 (IC50 7.21x10-8 M) SYBR Green assay [13]
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 37
pEC50 7.0 (EC50 1.1x10-7 M) [37]
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 38
pIC50 6.6 (IC50 2.5x10-7 M) SYBR green assay [38]
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 35
pIC50 7.1 (IC50 7.3x10-8 M) [3H]-hypoxanthine incorporation [35]
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 35
pIC50 6.7 (IC50 2.23x10-7 M) [3H]-hypoxanthine incorporation [35]
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 35
pIC50 5.4 (IC50 3.97x10-6 M) [3H]-hypoxanthine incorporation [35]
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 35
pIC50 8.4 (IC50 4x10-9 M) [3H]-hypoxanthine incorporation [35]
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 23
pEC50 5.8 (EC50 1.4x10-6 M) SYBR Green I assay [23]
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 23
pEC50 6.0 (EC50 9.7x10-7 M) SYBR Green I assay [23]
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 8
pIC50 8.4 (IC50 4x10-9 M) [3H]-hypoxanthine incorporation [8]
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 8
pIC50 9.0 (IC50 1x10-9 M) [3H]-hypoxanthine incorporation [8]
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 32
pIC50 7.3 (IC50 5.2x10-8 M) [3H]-hypoxanthine incorporation [32]
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 32
pIC50 7.7 (IC50 2x10-8 M) [3H]-hypoxanthine incorporation [32]
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 32
pIC50 7.4 (IC50 3.9x10-8 M) [3H]-hypoxanthine incorporation [32]
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 PfHB3 - 7.3 pIC50 32
pIC50 7.3 (IC50 5.6x10-8 M) [3H]-hypoxanthine incorporation [32]
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 PfFCR3 - 7.5 pIC50 32
pIC50 7.5 (IC50 3x10-8 M) [3H]-hypoxanthine incorporation [32]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum purine nucleoside phosphorylase forodesine Pf - 7.5 pIC50 19
pIC50 7.5 (IC50 3.5x10-8 M) Tran35S incorporation [19]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum purine nucleoside phosphorylase forodesine Pf - 9.2 pKi 18
pKi 9.2 (Ki 6x10-10 M) [18]
Plasmodium falciparum purine nucleoside phosphorylase mefloquine Pf - 5.2 pKi 9
pKi 5.2 (Ki 5.9x10-6 M) [9]
Plasmodium falciparum purine nucleoside phosphorylase quinine Pf - 6.9 pKi 9
pKi 6.9 (Ki 1.38x10-7 M) [9]
Plasmodium falciparum V-type proton ATPase MMV253 PfNF54 - 8.1 pIC50 11
pIC50 8.1 (IC50 9x10-9 M) SYBR Green assay [11]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum V-type proton ATPase MMV253 PfK1 - 7.8 pIC50 11
pIC50 7.8 (IC50 1.5x10-8 M) SYBR Green assay [11]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum heme detoxification protein compound 3a [PMID: 30344903] PfK1 - 7.3 pIC50 30
pIC50 7.3 (IC50 4.5x10-8 M) Parasite lactate dehydrogenase (pLDH) assay [30]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Plasmodium falciparum heme detoxification protein compound 3a [PMID: 30344903] PfFCR3 - 7.7 pIC50 30
pIC50 7.7 (IC50 2x10-8 M) Parasite lactate dehydrogenase (pLDH) assay [30]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA azithromycin Pf3D7 - 7.3 pIC50 6
pIC50 7.3 (IC50 5.27x10-8 M) FACS analysis following 96 hours in culture (third-generation rings) [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (96 hours)
Unknown MOA ganaplacide Pf3D7 - 8.1 pIC50 20
pIC50 8.1 (IC50 9x10-9 M) SYBR Green assay [20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA doxycycline Pf3D7 - 7.3 pIC50 6
pIC50 7.3 (IC50 4.53x10-8 M) FACS analysis following 96 hours in culture (third-generation rings) [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (96 hours)
Unknown MOA OSM-S-38 Pf3D7 - 8.4 pIC50 36
pIC50 8.4 (IC50 4x10-9 M) [36]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite late stage (IV–V) gametocyte assay
Unknown MOA SC83288 Pf3D7 - 8.1 pIC50 25
pIC50 8.1 (IC50 8x10-9 M) [25]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA AN13762 Pf3D7 - 7.4 pIC50 40
pIC50 7.4 (IC50 4.3x10-8 M) [3H]-hypoxanthine incorporation [40]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA azithromycin Pf3D7 - 5.1 pIC50 6
pIC50 5.1 (IC50 8.67x10-6 M) FACS analysis following 48 hours in culture (second-generation rings) [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (48 hours)
Unknown MOA OSM-S-38 Pf3D7 - 7.1 pIC50 36
pIC50 7.1 (IC50 7.9x10-8 M) [36]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA doxycycline Pf3D7 - 6.3 pIC50 6
pIC50 6.3 (IC50 5.32x10-7 M) FACS analysis following 48 hours in culture (second-generation rings) [6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (48 hours)
Unknown MOA ganaplacide PfNF54 - - - 20
Giemsa-stained blood film counts: potent inhibiton of gametocyte maturation at concentrations as low as 50 nM [20]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte maturation assay
Oocyst count: >90% reduction of oocyst numbers at a concentration of 500 nM [20]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
Unknown MOA artenimol PfNF54 - 9.0 pIC50 7
pIC50 9.0 (IC50 1.1x10-9 M) [3H]-hypoxanthine incorporation [7]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA primaquine PfNF54 - 5.9 pIC50 7
pIC50 5.9 (IC50 1.191x10-6 M) [3H]-hypoxanthine incorporation [7]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA artemisinin PfNF54 - 8.2 pIC50 7
pIC50 8.2 (IC50 5.8x10-9 M) [3H]-hypoxanthine incorporation [7]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA artefenomel PfNF54 - 8.7 pIC50 5
pIC50 8.7 (IC50 1.9x10-9 M) [3H]-hypoxanthine incorporation [5]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA mepacrine PfNF54 - 8.1 pIC50 10
pIC50 8.1 (IC50 8.3x10-9 M) [3H]-hypoxanthine incorporation [10]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA mefloquine PfNF54 - 8.0 pIC50 7
pIC50 8.0 (IC50 1.07x10-8 M) [3H]-hypoxanthine incorporation [7]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
Unknown MOA piperaquine