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ChEMBL ligand: CHEMBL1107 (DL-WR-171669, Halofantrine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 |
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 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]