- Guide to PHARMACOLOGY
Synonyms: Tikosyn® | UK-68798
dofetilide is an approved drug (FDA (1999))
Compound class: Synthetic organic
Comment: Dofetilide blocks potassium voltage-gated channels (HERGs).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Gómez-Varela D, Contreras-Jurado C, Furini S, García-Ferreiro R, Stühmer W, Pardo LA. (2006)
Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.
FEBS Lett, 580 (21): 5059-66. [PMID:16949586]
2. Singleton DH, Boyd H, Steidl-Nichols JV, Deacon M, Groot MJ, Price D, Nettleton DO, Wallace NK, Troutman MD, Williams C et al.. (2007)
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
J Med Chem, 50 (13): 2931-41. [PMID:17536794]