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Plasmodium berghei

Help on GtoMPdb Target Species Data

The GtoMPdb includes species information for antimalarial ligands and their target interactions.

Each individual Malaria Target Species page provides a detailed description of the species and a table displaying all interactions (contained in the database) associated with it.

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Species ID:109
Name:Plasmodium berghei
Associated with:10 targets
13 ligands
Description
P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.

Interactions

Interactions
Key to terms and symbols Click column headers to sort
Target Ligand Sp. Action Value Parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase DSM705 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 7.9 pEC50 9
pEC50 7.9 (EC50 1.3x10-8 M) Luciferase bioluminescence (Pbluc) assay to measure sporozoite invasion into HepG2 liver cells (prophylactic activity) [9]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD3444 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.8 pEC50 7
pEC50 6.8 (EC50 1.4x10-7 M) Luciferase bioluminescence assay to measure parasite invasion into HepG2 liver cells [7]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit BRD7929 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.8 pEC50 7
pEC50 6.8 (EC50 1.62x10-7 M) Luciferase bioluminescence assay to measure parasite invasion into HepG2 liver cells [7]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum N-myristoyltransferase compound 34c [PMID: 24641010] Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.4 pEC50 10
pEC50 6.4 (EC50 3.72x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [10]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum phosphatidylinositol 4-kinase beta UCT943 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 9.0 pIC50 3
pIC50 9.0 (IC50 9.2x10-10 M) Luciferase bioluminescence assay to measure sporozoite invasion (prophylactic activity) [3]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum elongation factor 2 M5717 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 8.8 pEC50 2
pEC50 8.8 (EC50 1.65x10-9 M) P. berghei Luciferase liver stage assay [2]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cGMP-dependent protein kinase MMV030084 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.7 pIC50 11
pIC50 6.7 (IC50 1.99x10-7 M) Luciferase bioluminescence assay to measure sporozoite invasion into HepG2 liver cells (prophylactic activity) [11]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum prolyl-tRNA synthetase halofuginone Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 7.8 pIC50 4
pIC50 7.8 (IC50 1.7x10-8 M) [4]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum histone deacetylase 1 compound 1u [PMID: 30245402] Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 7.6 pIC50 5
pIC50 7.6 (IC50 2.5x10-8 M) P. berghei Luciferase liver stage assay [5]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cytochrome b ELQ-300 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 9.0 pEC50 8
pEC50 9.0 (EC50 1.02x10-9 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms [8]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cytochrome b compound 27 [PMID: 32945666] Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.5 pIC50 6
pIC50 6.5 (IC50 3x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [6]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cyclin-dependent-like kinase CLK3 TCMDC-135051 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 6.4 pEC50 1
pEC50 6.4 (EC50 4x10-7 M) [1]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Unknown MOA OSM-S-38 Pb

Plasmodium berghei

P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa.
Pb is used in rodent model studies of malaria.
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 - 7.7 pIC50 12
pIC50 7.7 (IC50 1.9x10-8 M) [12]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay

References

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1. Alam MM, Sanchez-Azqueta A, Janha O, Flannery EL, Mahindra A, Mapesa K, Char AB, Sriranganadane D, Brancucci NMB, Antonova-Koch Y et al.. (2019) Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science, 365 (6456). [PMID:31467193]

2. Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G et al.. (2015) A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature, 522 (7556): 315-20. [PMID:26085270]

3. Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT et al.. (2018) UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria. Antimicrob Agents Chemother, 62 (9). [PMID:29941635]

4. Derbyshire ER, Mazitschek R, Clardy J. (2012) Characterization of Plasmodium liver stage inhibition by halofuginone. ChemMedChem, 7 (5): 844-9. [PMID:22438279]

5. Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T et al.. (2018) One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. Eur J Med Chem, 158: 801-813. [PMID:30245402]

6. Eagon S, Hammill JT, Sigal M, Ahn KJ, Tryhorn JE, Koch G, Belanger B, Chaplan CA, Loop L, Kashtanova AS et al.. (2020) Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-b]pyridines. J Med Chem, 63 (20): 11902-11919. [PMID:32945666]

7. Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V et al.. (2016) Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature, 538 (7625): 344-349. [PMID:27602946]

8. Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE et al.. (2013) Quinolone-3-diarylethers: a new class of antimalarial drug. Sci Transl Med, 5 (177): 177ra37. [PMID:23515079]

9. Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J et al.. (2021) Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem, 64 (9): 6085-6136. [PMID:33876936]

10. Rackham MD, Brannigan JA, Rangachari K, Meister S, Wilkinson AJ, Holder AA, Leatherbarrow RJ, Tate EW. (2014) Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). J Med Chem, 57 (6): 2773-88. [PMID:24641010]

11. Vanaerschot M, Murithi JM, Pasaje CFA, Ghidelli-Disse S, Dwomoh L, Bird M, Spottiswoode N, Mittal N, Arendse LB, Owen ES et al.. (2020) Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity. Cell Chem Biol, 27 (7): 806-816.e8. [PMID:32359426]

12. Williamson AE, Ylioja PM, Robertson MN, Antonova-Koch Y, Avery V, Baell JB, Batchu H, Batra S, Burrows JN, Bhattacharyya S et al.. (2016) Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles. ACS Cent Sci, 2 (10): 687-701. [PMID:27800551]