pyronaridine [Ligand Id: 10086] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL35228 (Pyronaridine)
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.19 pIC50 64000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL OSM: Late stage gametocytes. IC50 values determined from 21 point dose response curves. Avery Group Griffith. F 5.53 pIC50 2960 nM IC50 Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method F 5.77 pIC50 1710 nM IC50 Eur J Med Chem (2018) 158: 801-813 [PMID:30245402]
ChEMBL Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based confocal microplate imaging method F 6.85 pIC50 140 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 6.88 pIC50 131.3 nM IC50 J. Med. Chem. (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay F 7.34 pIC50 46 nM IC50 J. Med. Chem. (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method F 7.54 pIC50 29 nM IC50 Eur J Med Chem (2018) 158: 801-813 [PMID:30245402]
ChEMBL Antimalarial activity against transgenic Plasmodium falciparum 3D7 GFP16B gametocytes F 7.64 pIC50 23 nM IC50 J. Med. Chem. (2012) 55: 10328-10344 [PMID:23075290]
ChEMBL Antimalarial activity against Plasmodium falciparum KT3 gametocytes F 7.7 pIC50 20 nM IC50 J. Med. Chem. (2012) 55: 10328-10344 [PMID:23075290]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 measured after 72 hrs by DAPI staining based high throughput screening assay F 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antiplasmodial activity against 4-aminoquinoline/antifolates-resistant Plasmodium falciparum Dd2 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 7.74 pIC50 18 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method F 7.92 pIC50 12 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 7.92 pIC50 12 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 measured after 72 hrs by DAPI staining based high throughput screening assay F 7.92 pIC50 11.9 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.1 pIC50 8 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 8.12 pIC50 7.51 nM IC50 J. Nat. Prod. (2015) 78: 2932-2939 [PMID:26651537]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 8.12 pIC50 7.5 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL Antimalarial activity against Plasmodium falciparum KT1 gametocytes F 8.22 pIC50 6 nM IC50 J. Med. Chem. (2012) 55: 10328-10344 [PMID:23075290]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 8.44 pIC50 3.6 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL OSM: Inhibition of Plasmodium falciparum 3D7 growth. IC50 values determined from 21 point dose response curves. Avery Group Griffith. F 8.49 pIC50 3.2 nM IC50 Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
ChEMBL Inhibitory concentration IC50 against Plasmodium falciparum K1 by [3H]hypoxanthine uptake over 24 hr F 8.57 pIC50 2.7 nM IC50 J. Med. Chem. (1994) 37: 1486-1494 [PMID:8182707]
ChEMBL Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.72 pIC50 1.92 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antimalarial activity against Plasmodium falciparum at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.8 pIC50 1.6 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Inhibitory concentration against Plasmodium falciparum D6 infected erythrocytes F 9 pIC50 1 nM IC50 J. Med. Chem. (1994) 37: 1486-1494 [PMID:8182707]
ChEMBL Inhibitory concentration against Plasmodium falciparum W2 infected erythrocytes F 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (1994) 37: 1486-1494 [PMID:8182707]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 harboring pfs16-LUC-GFP late stage 4 to 5 gametocytes after 48 hrs by MitoTracker Red staining based confocal microscopy F 5.85 pEC50 1400 nM EC50 J Med Chem (2017) 60: 1171-1188 [PMID:28080063]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 harboring pfs16-LUC-GFP early stage 1 to 3 gametocytes after 48 hrs by MitoTracker Red staining based confocal microscopy F 7.6 pEC50 25 nM EC50 J Med Chem (2017) 60: 1171-1188 [PMID:28080063]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 harboring pfs16-LUC-GFP ring stage gametocytes after 24 hrs by MitoTracker Red staining based confocal microscopy F 7.8 pEC50 16 nM EC50 J Med Chem (2017) 60: 1171-1188 [PMID:28080063]
Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method F 8.24 pIC50 5.7 nM IC50 Med Chem Res (2007) 16: 213-229
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 8.44 pIC50 3.6 nM IC50 J. Nat. Prod. (2015) 78: 2932-2939 [PMID:26651537]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method F 8.04 pIC50 9.1 nM IC50 Med Chem Res (2007) 16: 213-229
Plasmodium falciparum NF54 (target type: ORGANISM) [ChEMBL: CHEMBL2367131]
ChEMBL Antimalarial activity against late stage gametocyte stage of Plasmodium falciparum NF54 after 72 hrs F 5.57 pIC50 2700 nM IC50 Eur. J. Med. Chem. (2014) 82: 204-213 [PMID:24904967]
Plasmodium malariae (target type: ORGANISM) [ChEMBL: CHEMBL613257]
ChEMBL Antimalarial activity against Plasmodium malariae trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay F 8.11 pIC50 7.8 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 197-202 [PMID:20937779]
ChEMBL Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay F 8.39 pIC50 4.1 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 197-202 [PMID:20937779]
Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013]
ChEMBL Antimalarial activity against Plasmodium vivax trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.33 pIC50 4.7 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.59 pIC50 2.58 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antimalarial activity against Plasmodium vivax at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.6 pIC50 2.5 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antimalarial activity against Plasmodium vivax with >50% parasites at ring stage infected in human erythrocytes assessed as growth inhibition after 30 to 50 hrs by microscopic analysis using giemsa staining F 8.62 pIC50 2.4 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin F 6 pIC50 <1000 nM IC50 J. Med. Chem. (2013) 56: 7761-7771 [PMID:23927658]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]