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ChEMBL ligand: CHEMBL35228 (Malaridine, Pyronaridine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 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 | 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 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 | Antiplasmodial activity against drug-resistant Plasmodium falciparum Dd2 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis | F | 7.96 | pIC50 | 11 | nM | IC50 | J Nat Prod (2019) 82: 1019-1023 [PMID:30865443] |
ChEMBL | Antimalarial activity against synchronous ring stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis | F | 8.08 | pIC50 | 8.3 | nM | IC50 | Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708] |
ChEMBL | Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis | F | 8.09 | pIC50 | 8.2 | nM | IC50 | J Nat Prod (2019) 82: 1019-1023 [PMID:30865443] |
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 | Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based confocal imaging analysis | F | 8.1 | pIC50 | 7.9 | nM | IC50 | J Med Chem (2019) 62: 622-640 [PMID:30537832] |
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 chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by DAPI staining based fluorescence assay | F | 8.12 | pIC50 | 7.5 | nM | IC50 | J Nat Prod (2020) 83: 316-322 [PMID:32067457] |
ChEMBL | Antimalarial activity against synchronous ring stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis | F | 8.13 | pIC50 | 7.4 | nM | IC50 | Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708] |
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis | F | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2019) 62: 622-640 [PMID:30537832] |
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 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite rowth incubated for 72 hrs by DAPI staining based fluorescence assay | F | 8.44 | pIC50 | 3.6 | nM | IC50 | J Nat Prod (2020) 83: 316-322 [PMID:32067457] |
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 | Antiplasmodial activity against late stage (IV/V) Plasmodium falciparum NF54 gametocytes transfected with GFP-LUC assessed as growth inhibition incubated for 72 hrs by mitotracker Red-CMXROS dye based fluorescence microscopic analysis | F | 5.51 | pEC50 | 3108 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
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 late stage (1 to 3) expressing Pfs16-LUC-GFP assessed as growth inhibition by high content imaging assay | F | 5.91 | pEC50 | 1240 | nM | EC50 | Eur J Med Chem (2021) 214: 113253-113253 [PMID:33610028] |
ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 early stage (1 to 3) expressing Pfs16-LUC-GFP assessed as growth inhibition by high content imaging assay | F | 7.28 | pEC50 | 53 | nM | EC50 | Eur J Med Chem (2021) 214: 113253-113253 [PMID:33610028] |
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]