Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug…
By W. Redfern, L. Carlsson, A. S. Davis, W. G. Lynch, I. Mackenzie, S. Palethorpe, P. Siegl, I. Strang, A. Sullivan, R. Wallis and 2 more. Cardiovascular Research, 2003
1,497 citations recorded by the source corpus.
Subfields: Cardiology and Cardiovascular Medicine, Molecular Biology
View Paper: https://www.semanticscholar.org/paper/1ca175c69cd591a2f6346cd41161682a367b502c
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In Molecular Biology
Citations in the corpus
- Compilation and physicochemical classification analysis of a diverse hERG inhibition database (2016, neutral): “It turned out that hERG exhibits very broad ligand specificity, so that long QT syndrome can be caused by a wide spectrum of drugs prescribed for a variety of therapeutic conditions [3, 4].”
- The influence of lipophilicity in drug discovery and design (2012, background): “Meaning that lipophilic basic molecules demonstrate the lowest probability to achieve a hERG IC50 of > 10 μM with lipophilitic acids, neutral compounds and zwitterions having a wider acceptable range of log P and log D and being considerably less problematic in this type of drug-induced toxicity [22”
- Medicinal chemical properties of successful central nervous system drugs (2005, background): “better risk assessment, a more than 30-fold margin between hERG IC50 and effective unbound plasma concentrations are recommended for drugs in clinical development.(71) It needs to be pointed out that challenge is to minimize hERG activity to eliminate a major risk factor, but not at the expense of d”
- Lipophilicity in drug discovery (2010, background): “The hERG cardiac potassium channel is well known for its promiscuity and ability to bind a variety of different chemotypes at a level of potency that is likely to become problematic [59].”