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