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ChEMBL ligand: CHEMBL652 (Flecainide, NSC-719273, THN-102 COMPONENT FLECAINIDE) |
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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 Potassium channel HERG expressed in mammalian cells | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human ERG | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
Kv4.2/Potassium voltage-gated channel subfamily D member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075227] [GtoPdb: 553] [UniProtKB: Q63881] | ||||||||
ChEMBL | Inhibition of rat potassium channel Kv4.2 by patch-clamp method | B | 5 | pIC50 | 10100 | nM | IC50 | J Med Chem (2007) 50: 2818-2841 [PMID:17506538] |
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
ChEMBL | Inhibition of human heart sodium channel Nav1.5 by patch-clamp method | B | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (2007) 50: 2818-2841 [PMID:17506538] |
Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460] | ||||||||
GtoPdb | - | - | 4 | pKd | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
ChEMBL | Inhibition of human potassium channel Kv1.5 by patch-clamp method | B | 4.29 | pIC50 | 51000 | nM | IC50 | J Med Chem (2007) 50: 2818-2841 [PMID:17506538] |
Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388] | ||||||||
GtoPdb | - | - | 3.7 | pKd | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142] | ||||||||
GtoPdb | - | - | 3.7 | pKd | 217000 | nM | Kd | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
Kv1.7 in Human [GtoPdb: 544] [UniProtKB: Q96RP8] | ||||||||
GtoPdb | - | - | 5.1 | pKd | - | - | - | Eur J Hum Genet (2002) 10: 36-43 [PMID:11896454] |
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388] | ||||||||
GtoPdb | - | - | 4 | pIC50 | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
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]