a curated resource for data describing chemical triggered in vitro cardiac ion channels inhibition

Sebastian Polak, Barbara Wiśniowska, Anna Glinka, Miłosz Polak
2012 BMC Pharmacology and Toxicology  
Drugs safety issues are now recognized as being factors generating the most reasons for drug withdrawals at various levels of development and at the post-approval stage. Among them cardiotoxicity remains the main reason, despite the substantial effort put into in vitro and in vivo testing, with the main focus put on hERG channel inhibition as the hypothesized surrogate of drug proarrhythmic potency. The large interest in the IKr current has resulted in the development of predictive tools and
more » ... ormative databases describing a drug's susceptibility to interactions with the hERG channel, although there are no similar, publicly available sets of data describing other ionic currents driven by the human cardiomyocyte ionic channels, which are recognized as an overlooked drug safety target. Discussion: The aim of this database development and publication was to provide a scientifically useful, easily usable and clearly verifiable set of information describing not only IKr (hERG), but also other human cardiomyocyte specific ionic channels inhibition data (IKs, INa, ICa). Summary: The broad range of data (chemical space and in vitro settings) and the easy to use user interface makes a useful tool for interested scientists. Database URL:
doi:10.1186/2050-6511-13-6 pmid:22947121 pmcid:PMC3506270 fatcat:lwsy5surjzcu7f5ougyd375nvi