disopyramide [Ligand Id: 7167] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL517 (H-3292, Disopyramide, SC-7031, Norpace)
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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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]
GtoPdb - - 4.04 pIC50 91201 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-5 [PMID:12873512]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.04 pIC50 91201.08 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.04 pIC50 91201.08 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 4.04 pIC50 91201.08 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 4.04 pIC50 91201.08 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against IKr potassium channel B 4.92 pIC50 12000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.09 pIC50 81700 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cells F 4.21 pKi 62000 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cells F 4.52 pKi 30000 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]