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Plasmodium berghei

Species ID:109
Name:Plasmodium berghei
Associated with:8 targets
10 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 - 7.9 pEC50 7
pEC50 7.9 (EC50 1.3x10-8 M) Luciferase bioluminescence (Pbluc) assay to measure sporozoite invasion into HepG2 liver cells (prophylactic activity) [7]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum glycylpeptide N-tetradecanoyltransferase compound 34c [PMID: 24641010] Pb - 6.4 pEC50 8
pEC50 6.4 (EC50 3.72x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [8]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum phosphatidylinositol 4-kinase UCT943 Pb - 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 - 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 - 6.7 pIC50 9
pIC50 6.7 (IC50 1.99x10-7 M) Luciferase bioluminescence 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 histone deacetylase 1 compound 1u [PMID: 30245402] Pb - 7.6 pIC50 4
pIC50 7.6 (IC50 2.5x10-8 M) P. berghei Luciferase liver stage assay [4]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cytochrome b ELQ-300 Pb - 9.0 pEC50 6
pEC50 9.0 (EC50 1.02x10-9 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms [6]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum cytochrome b compound 27 [PMID: 32945666] Pb - 6.5 pIC50 5
pIC50 6.5 (IC50 3x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [5]
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 - 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 - 7.7 pIC50 10
pIC50 7.7 (IC50 1.9x10-8 M) [10]
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. 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]

5. 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]

6. 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]

7. 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]

8. 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]

9. 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]

10. 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]