Plasmodium falciparum dihydroorotate dehydrogenase
|
DSM421
|
|
|
|
|
|
|
|
|
|
|
-
|
7.4 – 7.8
|
pEC50 |
20 |
|
pEC50
7.8
(EC50 1.4x10-8 M)
SYBR Green incorporation (72h assay)
[20]
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)
[20]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum dihydroorotate dehydrogenase
|
DSM265
|
|
|
|
|
|
|
|
|
|
|
-
|
7.5
|
pIC50 |
19 |
|
pIC50
7.5
(IC50 3x10-8 M)
[3H]-hypoxanthine incorporation
[19]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum dihydroorotate dehydrogenase
|
DSM421
|
|
|
|
|
|
|
|
|
|
|
Inhibition
|
7.3
|
pIC50 |
20 |
|
pIC50
7.3
(IC50 5.3x10-8 M)
[20]
Description: Steady-state kinetic analysis of recombinant enzyme inhibition.
|
Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit
|
BRD3444
|
|
|
|
|
|
|
|
|
|
|
Inhibition
|
7.3
|
pIC50 |
13 |
|
pIC50
7.3
(IC50 4.6x10-8 M)
[13]
|
Plasmodium falciparum N-Myristoyltransferase
|
Compound 34c [PMID 24641010]
|
|
|
|
|
|
|
|
|
|
|
-
|
6.5
|
pEC50 |
21 |
|
pEC50
6.5
(EC50 3.02x10-7 M)
[3H]-hypoxanthine incorporation
[21]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum N-Myristoyltransferase
|
Compound 34c [PMID 24641010]
|
|
|
|
|
|
|
|
|
|
|
Inhibition
|
8.1
|
pKi |
21 |
|
pKi
8.1
(Ki 8x10-9 M)
[21]
Description: Enzyme inhibition assay
|
Plasmodium falciparum N-Myristoyltransferase
|
Compound 34c [PMID 24641010]
|
|
|
|
|
|
|
|
|
|
|
-
|
6.6
|
pEC50 |
21 |
|
pEC50
6.6
(EC50 2.32x10-7 M)
[3H]-hypoxanthine incorporation
[21]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum N-Myristoyltransferase
|
Compound 34c [PMID 24641010]
|
|
|
|
|
|
|
|
|
|
|
-
|
6.5
|
pEC50 |
21 |
|
pEC50
6.5
(EC50 3.39x10-7 M)
[3H]-hypoxanthine incorporation
[21]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum N-Myristoyltransferase
|
Compound 34c [PMID 24641010]
|
|
|
|
|
|
|
|
|
|
|
-
|
6.0
|
pEC50 |
21 |
|
pEC50
6.0
(EC50 9.16x10-7 M)
[3H]-hypoxanthine incorporation
[21]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
(+)-SJ733
|
|
|
|
|
|
|
|
|
|
|
-
|
7.5
|
pEC50 |
10 |
|
pEC50
7.5
(EC50 3x10-8 M)
SYBR Green I assay
[10]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pIC50 |
22 |
|
pIC50
9.1
(IC50 7x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
-
|
- |
24 |
|
Giemsa-stained blood film counts: dose-dependent, inhibition of stage V gametocyte development
[24]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite late stage (III–V) gametocyte assay
Oocyst count: significantly reduced count observed with the addition of cipargamin when compared to control feeds
[24]
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, significant inhibition of stage II gametocyte development
[24]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite early stage (I–II) gametocyte assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.3
|
pIC50 |
22 |
|
pIC50
9.3
(IC50 5x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
(+)-SJ733
|
|
|
|
|
|
|
|
|
|
|
-
|
7.2
|
pEC50 |
10 |
|
pEC50
7.2
(EC50 6x10-8 M)
SYBR Green I assay
[10]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
8.9
|
pIC50 |
22 |
|
pIC50
8.9
(IC50 1.4x10-9 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
MMV253
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
8 |
|
pIC50
8.1
(IC50 9x10-9 M)
SYBR Green assay
[8]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
(+)-SJ733
|
|
|
|
|
|
|
|
|
|
|
-
|
7.4
|
pEC50 |
10 |
|
pEC50
7.4
(EC50 4x10-8 M)
SYBR Green I assay
[10]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.2
|
pIC50 |
22 |
|
pIC50
9.2
(IC50 6x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.0
|
pIC50 |
22 |
|
pIC50
9.0
(IC50 1x10-9 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
8.9
|
pIC50 |
22 |
|
pIC50
8.9
(IC50 1.2x10-9 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pIC50 |
22 |
|
pIC50
9.1
(IC50 9x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.3
|
pIC50 |
22 |
|
pIC50
9.3
(IC50 5x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
cipargamin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pIC50 |
22 |
|
pIC50
9.1
(IC50 9x10-10 M)
[3H]-hypoxanthine incorporation assay
[22]
Description: Parasite growth inhibition assay
|
Plasmodium falciparum ATPase4
|
(+)-SJ733
|
|
|
|
|
|
|
|
|
|
|
-
|
7.7
|
pEC50 |
10 |
|
pEC50
7.7
(EC50 2x10-8 M)
SYBR Green I assay
[10]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV024101
|
|
|
|
|
|
|
|
|
|
|
-
|
6.2
|
pIC50 |
12 |
|
pIC50
6.2
(IC50 6x10-7 M)
[12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV048
|
|
|
|
|
|
|
|
|
|
|
-
|
6.6 – 6.7
|
pIC50 |
17 |
|
pIC50
6.7
(IC50 2.14x10-7 M)
Parasite early stage (I-III) gametocyte assay using luciferase reporter line
[17]
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
[17]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
compound 55 [PMID: 29889526]
|
|
|
|
|
|
|
|
|
|
|
-
|
7.2
|
pIC50 |
12 |
|
pIC50
7.2
(IC50 6.3x10-8 M)
[12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.3
|
pIC50 |
3 |
|
pIC50
8.3
(IC50 5.4x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV048
|
|
|
|
|
|
|
|
|
|
|
-
|
6.8
|
pIC50 |
17 |
|
pIC50
6.8
(IC50 1.4x10-7 M)
Parasite late stage (IV-V) gametocyte assay using luciferase reporter line
[17]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV024101
|
|
|
|
|
|
|
|
|
|
|
-
|
6.3
|
pIC50 |
12 |
|
pIC50
6.3
(IC50 5.43x10-7 M)
[12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV048
|
|
|
|
|
|
|
|
|
|
|
-
|
7.6
|
pIC50 |
17 |
|
pIC50
7.6
(IC50 2.8x10-8 M)
[3H]-hypoxanthine incorporation assay
[17]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
3 |
|
pIC50
8.4
(IC50 4.2x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
7.2
|
pIC50 |
3 |
|
pIC50
7.2
(IC50 6.6x10-8 M)
Parasite late stage (IV-V) gametocyte assay using luciferase reporter line
[3]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV048
|
|
|
|
|
|
|
|
|
|
|
-
|
6.9
|
pIC50 |
17 |
|
pIC50
6.9
(IC50 1.11x10-7 M)
Indirect SMFA
[17]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
6.9 – 7.1
|
pIC50 |
3 |
|
pIC50
7.1
(IC50 8x10-8 M)
Reports on the functional viability of male and female mature stage V gametocytes
[3]
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
[3]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite gametocyte viability assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
MMV048
|
|
|
|
|
|
|
|
|
|
|
Binding
|
6.5 – 7.0
|
pKd |
17 |
|
pKd
7.0
(Kd 1x10-7 M)
[17]
pKd
6.5
(Kd 3x10-7 M)
[17]
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.3
|
pIC50 |
3 |
|
pIC50
8.3
(IC50 4.7x10-9 M)
[3H]-hypoxanthine incorporation
[3]
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]
|
|
|
|
|
|
|
|
|
|
|
-
|
7.0
|
pIC50 |
12 |
|
pIC50
7.0
(IC50 1.02x10-7 M)
[12]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.3
|
pIC50 |
3 |
|
pIC50
8.3
(IC50 5.2x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
3 |
|
pIC50
8.4
(IC50 4.1x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.2
|
pIC50 |
3 |
|
pIC50
8.2
(IC50 5.7x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum phosphatidylinositol 4-kinase
|
UCT943
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
3 |
|
pIC50
8.4
(IC50 3.7x10-9 M)
[3H]-hypoxanthine incorporation
[3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum elongation factor 2
|
M5717
|
|
|
|
|
|
|
|
|
|
|
-
|
9.0
|
pEC50 |
1 |
|
pEC50
9.0
(EC50 1x10-9 M)
[3H]-hypoxanthine incorporation assay
[1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum elongation factor 2
|
M5717
|
|
|
|
|
|
|
|
|
|
|
-
|
8.0 – 8.9
|
pEC50 |
1 |
|
pEC50
8.9
(EC50 1.2x10-9 M)
Female gamete formation
[1]
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
[1]
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
[1]
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
[1]
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
|
|
|
|
|
|
|
|
|
|
|
-
|
6.5
|
pIC50 |
11 |
|
pIC50
6.5
(IC50 2.9x10-7 M)
[3H]-hypoxanthine incorporation assay
[11]
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
|
|
|
|
|
|
|
|
|
|
|
-
|
6.5
|
pIC50 |
11 |
|
pIC50
6.5
(IC50 3.5x10-7 M)
[3H]-hypoxanthine incorporation assay
[11]
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
|
|
|
|
|
|
|
|
|
|
|
-
|
6.4
|
pIC50 |
11 |
|
pIC50
6.4
(IC50 3.7x10-7 M)
[3H]-hypoxanthine incorporation assay
[11]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
6 |
|
pIC50
8.4
(IC50 4.5x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
<5.0
|
pIC50 |
6 |
|
pIC50
<5.0
(IC50 >1x10-5 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
P218
|
|
|
|
|
|
|
|
|
|
|
-
|
7.3
|
pIC50 |
28 |
|
pIC50
7.3
(IC50 5.6x10-8 M)
[3H]-hypoxanthine incorporation
[28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
6.3
|
pIC50 |
6 |
|
pIC50
6.3
(IC50 4.45x10-7 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
8.8
|
pIC50 |
6 |
|
pIC50
8.8
(IC50 1.7x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
6.4
|
pIC50 |
6 |
|
pIC50
6.4
(IC50 3.657x10-7 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
6.0
|
pIC50 |
6 |
|
pIC50
6.0
(IC50 1.002x10-6 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
cycloguanil
|
|
|
|
|
|
|
|
|
|
|
-
|
5.4
|
pIC50 |
6 |
|
pIC50
5.4
(IC50 4.262x10-6 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
pyrimethamine
|
|
|
|
|
|
|
|
|
|
|
-
|
7.2
|
pIC50 |
28 |
|
pIC50
7.2
(IC50 5.8x10-8 M)
[3H]-hypoxanthine incorporation assay wild-type P. falciparum (TM4)
[28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
|
P218
|
|
|
|
|
|
|
|
|
|
|
-
|
8.3
|
pIC50 |
28 |
|
pIC50
8.3
(IC50 4.6x10-9 M)
[3H]-hypoxanthine incorporation
[28]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum proline--tRNA ligase
|
halofuginone
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pEC50 |
9 |
|
pEC50
9.1
(EC50 8.6x10-10 M)
SYBR Green assay
[9]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum proline--tRNA ligase
|
halofuginone
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pEC50 |
9 |
|
pEC50
9.1
(EC50 8.1x10-10 M)
SYBR Green assay
[9]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
|
sulfadoxine
|
|
|
|
|
|
|
|
|
|
|
-
|
7.1
|
pIC50 |
26 |
|
pIC50
7.1
(IC50 7.3x10-8 M)
[3H]-hypoxanthine incorporation
[26]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
|
sulfadoxine
|
|
|
|
|
|
|
|
|
|
|
-
|
6.7
|
pIC50 |
26 |
|
pIC50
6.7
(IC50 2.23x10-7 M)
[3H]-hypoxanthine incorporation
[26]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
|
sulfadoxine
|
|
|
|
|
|
|
|
|
|
|
-
|
5.4
|
pIC50 |
26 |
|
pIC50
5.4
(IC50 3.97x10-6 M)
[3H]-hypoxanthine incorporation
[26]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
|
sulfadoxine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
26 |
|
pIC50
8.4
(IC50 4x10-9 M)
[3H]-hypoxanthine incorporation
[26]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
OSM-S-38
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
27 |
|
pIC50
8.4
(IC50 4x10-9 M)
[27]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite late stage (IV–V) gametocyte assay
|
Unknown MOA
|
SC83288
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
18 |
|
pIC50
8.1
(IC50 8x10-9 M)
[18]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
KAF156
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
14 |
|
pIC50
8.1
(IC50 9x10-9 M)
SYBR Green assay
[14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
doxycycline
|
|
|
|
|
|
|
|
|
|
|
-
|
7.3
|
pIC50 |
5 |
|
pIC50
7.3
(IC50 4.53x10-8 M)
FACS analysis following 96 hours in culture (third-generation rings)
[5]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (96 hours)
|
Unknown MOA
|
azithromycin
|
|
|
|
|
|
|
|
|
|
|
-
|
5.1 – 7.3
|
pIC50 |
5 |
|
pIC50
7.3
(IC50 5.27x10-8 M)
FACS analysis following 96 hours in culture (third-generation rings)
[5]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (96 hours)
pIC50
5.1
(IC50 8.67x10-6 M)
FACS analysis following 48 hours in culture (second-generation rings)
[5]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (48 hours)
|
Unknown MOA
|
doxycycline
|
|
|
|
|
|
|
|
|
|
|
-
|
6.3
|
pIC50 |
5 |
|
pIC50
6.3
(IC50 5.32x10-7 M)
FACS analysis following 48 hours in culture (second-generation rings)
[5]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Ring formation assay (48 hours)
|
Unknown MOA
|
OSM-S-38
|
|
|
|
|
|
|
|
|
|
|
-
|
7.1
|
pIC50 |
27 |
|
pIC50
7.1
(IC50 7.9x10-8 M)
[27]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
KAF156
|
|
|
|
|
|
|
|
|
|
|
-
|
-
|
- |
14 |
|
Oocyst count: >90% reduction of oocyst numbers at a concentration of 500 nM
[14]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
|
Unknown MOA
|
primaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
5.9
|
pIC50 |
6 |
|
pIC50
5.9
(IC50 1.191x10-6 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
mepacrine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
7 |
|
pIC50
8.1
(IC50 8.3x10-9 M)
[3H]-hypoxanthine incorporation
[7]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
mefloquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.0
|
pIC50 |
6 |
|
pIC50
8.0
(IC50 1.07x10-8 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
piperaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
6 |
|
pIC50
8.1
(IC50 8.3x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
SC83288
|
|
|
|
|
|
|
|
|
|
|
-
|
8.7
|
pIC50 |
18 |
|
pIC50
8.7
(IC50 2x10-9 M)
[18]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
halofantrine
|
|
|
|
|
|
|
|
|
|
|
-
|
9.1
|
pIC50 |
6 |
|
pIC50
9.1
(IC50 9x10-10 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
KAF156
|
|
|
|
|
|
|
|
|
|
|
-
|
7.8
|
pIC50 |
14 |
|
pIC50
7.8
(IC50 1.64x10-8 M)
SYBR Green assay
[14]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
amodiaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.4
|
pIC50 |
6 |
|
pIC50
8.4
(IC50 3.9x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artefenomel
|
|
|
|
|
|
|
|
|
|
|
-
|
8.7
|
pIC50 |
4 |
|
pIC50
8.7
(IC50 1.9x10-9 M)
[3H]-hypoxanthine incorporation
[4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artemisinin
|
|
|
|
|
|
|
|
|
|
|
-
|
8.2
|
pIC50 |
6 |
|
pIC50
8.2
(IC50 5.8x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artemether
|
|
|
|
|
|
|
|
|
|
|
-
|
8.5
|
pIC50 |
6 |
|
pIC50
8.5
(IC50 3.5x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artesunate
|
|
|
|
|
|
|
|
|
|
|
-
|
8.5
|
pIC50 |
6 |
|
pIC50
8.5
(IC50 3.5x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artenimol
|
|
|
|
|
|
|
|
|
|
|
-
|
9.0
|
pIC50 |
6 |
|
pIC50
9.0
(IC50 1.1x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
lumefantrine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.6
|
pIC50 |
6 |
|
pIC50
8.6
(IC50 2.8x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
ACT-451840
|
|
|
|
|
|
|
|
|
|
|
-
|
8.2 – 9.4
|
pIC50 |
15 |
|
pIC50
9.4
(IC50 4x10-10 M)
[3H]-hypoxanthine incorporation
[15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
pIC50
8.2
(IC50 5.89x10-9 M)
male gamete formation from the gametocyte stage
[15]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Description: Parasite dual gamete formation assay (DGFA)
Conditions: ACT-451840 had no effect on the functional viability of female gametocytes up to a concentration of 20 μM.
|
Unknown MOA
|
artemisinin
|
|
|
|
|
|
|
|
|
|
|
-
|
9.2
|
pIC50 |
6 |
|
pIC50
9.2
(IC50 6x10-10 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artemether
|
|
|
|
|
|
|
|
|
|
|
-
|
8.5
|
pIC50 |
6 |
|
pIC50
8.5
(IC50 2.9x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
ACT-451840
|
|
|
|
|
|
|
|
|
|
|
-
|
9.5
|
pIC50 |
15 |
|
pIC50
9.5
(IC50 3x10-10 M)
[3H]-hypoxanthine incorporation
[15]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
primaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
6.3
|
pIC50 |
6 |
|
pIC50
6.3
(IC50 5.427x10-7 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
halofantrine
|
|
|
|
|
|
|
|
|
|
|
-
|
9.5
|
pIC50 |
6 |
|
pIC50
9.5
(IC50 3x10-10 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
amodiaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.0
|
pIC50 |
6 |
|
pIC50
8.0
(IC50 9.4x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
piperaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.0
|
pIC50 |
6 |
|
pIC50
8.0
(IC50 1.05x10-8 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
lumefantrine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.9
|
pIC50 |
6 |
|
pIC50
8.9
(IC50 1.3x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artenimol
|
|
|
|
|
|
|
|
|
|
|
-
|
9.0
|
pIC50 |
6 |
|
pIC50
9.0
(IC50 1x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
artesunate
|
|
|
|
|
|
|
|
|
|
|
-
|
8.5
|
pIC50 |
6 |
|
pIC50
8.5
(IC50 3.1x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
mefloquine
|
|
|
|
|
|
|
|
|
|
|
-
|
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
|
Unknown MOA
|
artefenomel
|
|
|
|
|
|
|
|
|
|
|
-
|
-
|
- |
6 |
|
>60% inhibition of exflagellation following 24hour exposure of mature gametocytes to 10µM artefenomel
[6]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Parasite exflagellation assay
|
Unknown MOA
|
ACT-451840
|
|
|
|
|
|
|
|
|
|
|
-
|
7.5
|
pIC50 |
15 |
|
pIC50
7.5
(IC50 3x10-8 M)
Indirect mode: dose-dependent inhibition of oocyst development in the mosquito was observed. Direct mode: no activity at concentrations up to 1 μM
[15]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Description: Standard membrane feeding assay (SMFA)
|
Unknown MOA
|
ferroquine
|
|
|
|
|
|
|
|
|
|
|
-
|
9.4
|
pIC50 |
2 |
|
pIC50
9.4
(IC50 3.7x10-10 M)
[3H]-hypoxanthine incorporation. Strain SGE2 (Zaire) designated as chloroquine sensitive.
[2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
SC83288
|
|
|
|
|
|
|
|
|
|
|
-
|
8.3
|
pIC50 |
18 |
|
pIC50
8.3
(IC50 5x10-9 M)
[18]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
piperaquine
|
|
|
|
|
|
|
|
|
|
|
-
|
8.1
|
pIC50 |
6 |
|
pIC50
8.1
(IC50 9x10-9 M)
[3H]-hypoxanthine incorporation
[6]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Parasite growth inhibition assay
|
Unknown MOA
|
KAF156
|
|