Toward in vivo-relevant herg safety assessment and mitigation strategies based on relationships between non-equilibrium blocker binding, three-dimensional channel-blocker interactions, dynamic occupancy, dynamic exposure, and cellular arrhythmia

HIGHLIGHTS

• who: Hongbin Wan et al. from the (UNIVERSITY) have published the article: Toward in vivo-relevant hERG safety assessment and mitigation strategies based on relationships between non-equilibrium blocker binding, three-dimensional channel-blocker interactions, dynamic occupancy, dynamic exposure, and cellular arrhythmia, in the Journal: PLOS ONE of August/16,/2020
• what: The authors propose a two-step blocker binding process consisting of: 1. The status quo hERG safety index (SI) is based on an entirely empirical model (expressed as the maximum safe free plasma Cmax=1/30 hERG IC50) that the authors show in . . .
  

   

  

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