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

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ChEMBL ligand: CHEMBL652 (Flecainida, 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 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]