flecainide [Ligand Id: 2560] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL652 (Flecainide, NSC-719273, THN-102 COMPONENT FLECAINIDE)
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  • Kv4.2/Potassium voltage-gated channel subfamily D member 2 in Rat [ChEMBL: CHEMBL1075227] [GtoPdb: 553] [UniProtKB: Q63881]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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  • Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
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  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
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  • Kv1.7 in Human [GtoPdb: 544] [UniProtKB: Q96RP8]
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  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
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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 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]