halofantrine [Ligand Id: 10019] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1107 (Halofantrine)
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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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells B 5.12 pKi 7500 nM Ki ACS Med. Chem. Lett. (2013) 4: 1037-1041 [PMID:24900603]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.7 pIC50 199.53 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.7 pIC50 199.53 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 6.7 pIC50 199.53 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in MCF7 cells B 6.7 pIC50 199.53 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.7 pIC50 199.53 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.1 F 6.71 pIC50 196 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG B 6.71 pIC50 194.98 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG by fluorescence polarization assay B 6.81 pIC50 156 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Inhibition of human cloned ERG B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2009) 52: 1408-1415 [PMID:19222165]
ChEMBL Inhibitory concentration against IKr potassium channel B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
GtoPdb - - 7.4 pIC50 40 nM IC50 J. Med. Chem. (2009) 52: 1408-15 [PMID:19222165]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes F 8.03 pIC50 9.3 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 423-424 [PMID:11212126]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay F 8.05 pIC50 9 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 3131-3134 [PMID:19364853]
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 5.8 nM IC50 Med Chem Res (2007) 16: 213-229
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 8.55 pIC50 2.8 nM IC50 Med Chem Res (2007) 16: 213-229

ChEMBL data shown on this page come from version 26:

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]