flecainide [Ligand Id: 2560] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL652 (Flecainida, Flecainide, Flecainide component of thn102, FLECAINIDE COMPONENT OF THN-102, NSC-719273) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv4.2/A-type voltage-gated potassium channel KCND2 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] |
| Kv1.5/Potassium voltage-gated channel subfamily A member 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] |
| Nav1.5/Sodium channel protein type 5 subunit alpha 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] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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] |
| 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 36:
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]
