dronedarone [Ligand Id: 7465] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL184412 (Dronedarone, SR33589, SR-33589)
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
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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 Inhibitory concentration against IKr potassium channel B 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG B 6.5 pIC50 316.23 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes F 6.4 pIC50 400 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb Whole cell patch clamp experiment using HEK293 cells expressing human Kv1.5. - 5.63 pIC50 2370 nM IC50 Eur J Med Chem (2014) 81: 89-94 [PMID:24824064]

ChEMBL data shown on this page come from version 27:

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]