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ChEMBL ligand: CHEMBL566534 (Artemetero, Artemether, Artemetheri, Artemetherum, Artesaph, .beta.-artemether, Dihydroartemisinin impurity g, Falcidol, Gvither, Larither, Malartem, NSC-665970, NSC-759820, Paluther, SM 224, SM224) |
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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 berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
ChEMBL | In vivo antimalarial activity against Plasmodium berghei infected mouse model assessed as parasitemia at 8 mg/kg, po in presence of Mefloquine hydrochloride | F | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2016) 59: 7360-7388 [PMID:27010926] |
ChEMBL | Antiplasmodial activity against Plasmodium berghei ANKA early trophozoite stage by parasite LDH assay | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2015) 58: 7895-7899 [PMID:26367273] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs | F | 4.19 | pIC50 | >64000 | nM | IC50 | Bioorg Med Chem (2014) 22: 5241-5248 [PMID:25199582] |
ChEMBL | In vitro anti-protozoal activity against Plasmodium falciparum Ghana | F | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2013-2015 [PMID:12781185] |
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O-positive erythrocytes assessed as decrease in parasitaemia after 72 hrs by NBT dye-based spectrophotometric method | F | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2018) 143: 306-319 [PMID:29197735] |
ChEMBL | In vitro antimalarial activity against Plasmodium falciparum FCR3 | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 75-77 [PMID:12467620] |
ChEMBL | In vitro inhibitory concentration against chloroquine-sensitive Plasmodium falciparum HB3 | F | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2002) 45: 1052-1063 [PMID:11855985] |
ChEMBL | Antimalarial activity against Plasmodium falciparum K1 | F | 8.05 | pIC50 | 9 | nM | IC50 | Eur J Med Chem (2021) 213: 113193-113193 [PMID:33508479] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 8.1 | pIC50 | 7.94 | nM | IC50 | Eur J Med Chem (2021) 213: 113193-113193 [PMID:33508479] |
ChEMBL | In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum K1 | F | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2002) 45: 1052-1063 [PMID:11855985] |
ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay | F | 8.14 | pIC50 | 7.26 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430] |
ChEMBL | Antimalarial activity against Plasmodium falciparum W2 | F | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2021) 213: 113193-113193 [PMID:33508479] |
ChEMBL | In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum K1 | F | 8.19 | pIC50 | 6.5 | nM | IC50 | J Med Chem (2002) 45: 1052-1063 [PMID:11855985] |
ChEMBL | Antimalarial activity against chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay | F | 8.24 | pIC50 | 5.77 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430] |
ChEMBL | In vitro inhibitory activity against the chloroquine-resistant Plasmodium falciparum W2 Indochina | F | 8.27 | pIC50 | 5.4 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1059-1062 [PMID:12643911] |
ChEMBL | In vitro antimalarial activity for Plasmodium falciparum W-2 | F | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (1998) 41: 4101-4108 [PMID:9767645] |
ChEMBL | In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 8.34 | pIC50 | 4.55 | nM | IC50 | J Med Chem (2001) 44: 58-68 [PMID:11141088] |
ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay | F | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430] |
ChEMBL | Inhibitory concentration against Plasmodium falciparum D6 (Sierra Leone) | F | 8.35 | pIC50 | 4.49 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as growth inhibition by [3H]hypoxanthine incorporation assay | F | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2010) 53: 633-640 [PMID:19957999] |
ChEMBL | Antiplasmodial activity against chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 measured after 48 hrs by pLDH assay | F | 8.42 | pIC50 | 3.8 | nM | IC50 | Eur J Med Chem (2016) 122: 635-646 [PMID:27448920] |
ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay | F | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127581-127581 [PMID:32987134] |
ChEMBL | Antimalarial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | F | 8.45 | pIC50 | 3.53 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2033-2037 [PMID:19249201] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | F | 8.45 | pIC50 | 3.53 | nM | IC50 | Bioorg Med Chem (2009) 17: 1325-1338 [PMID:19136263] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum FCB1 assessed as inhibition of parasite growth | F | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
ChEMBL | In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum FcB1 | F | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2004) 47: 1423-1433 [PMID:14998331] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake | F | 8.46 | pIC50 | 3.45 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2038-2043 [PMID:19251414] |
ChEMBL | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 | F | 8.47 | pIC50 | 3.42 | nM | IC50 | J Med Chem (2001) 44: 58-68 [PMID:11141088] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 (Thailand) assessed as growth inhibition by [3H]hypoxanthine incorporation assay | F | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2010) 53: 633-640 [PMID:19957999] |
ChEMBL | Inhibitory concentration against Plasmodium falciparum W2 Indochina | F | 8.48 | pIC50 | 3.34 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 | F | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1720-1724 [PMID:18243702] |
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 | F | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2008) 51: 2170-2177 [PMID:18341274] |
ChEMBL | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2008) 51: 1260-1277 [PMID:18260613] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 8.6 | pIC50 | 2.5 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1291-1296 [PMID:18268087] |
ChEMBL | Intrinsic equimolar activity against Plasmodium falciparum D6 (Sierra Leone) relative to QHS | F | 8.63 | pIC50 | 2.34 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by LDH assay | F | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127581-127581 [PMID:32987134] |
ChEMBL | Antiplasmodial activity against chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 measured after 48 hrs by pLDH assay | F | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2016) 122: 635-646 [PMID:27448920] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | F | 8.68 | pIC50 | 2.11 | nM | IC50 | Bioorg Med Chem (2009) 17: 1325-1338 [PMID:19136263] |
ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 | F | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2021) 213: 113193-113193 [PMID:33508479] |
ChEMBL | Intrinsic equimolar activity against Plasmodium falciparum W2 Indochina relative to QHS | F | 8.72 | pIC50 | 1.92 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected human erythrocytes after 24 hrs by [3H]hypoxanthine uptake | F | 8.9 | pIC50 | 1.26 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5804-5804 [PMID:18845438] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake | F | 8.9 | pIC50 | 1.26 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2038-2043 [PMID:19251414] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]