hERG inhibition leading to cardiac toxicity

hERG channel blockade leading to sudden cardiac death

Increased mortality triggered by drug-mediated blockade of human ether-a-gogo-related gene (hERG) channel. The inhibition of rapid delayed rectifying potassium current, prolongation of action potential duration, prolongation of QT interval, and Torsades de Pointes. Overall, all these steps indicate that there has been a disruption in cardiac electrophysiology, leading to sudden cardiac death on an individual level.

Data: ID (ChEMBL240) assigned to the hERG channel. To ensure data validity, the database was mined retaining only those entries matching the following criteria already suggested in the literature: 1) annotated exclusively with IC50 (11,144 entries) measures, 2) referring to assays conducted on human targets (“target_organism” = “Homo sapiens”), 3) marked as direct binding (“assay_type” = “B”), and 4) free of warnings in the “data_validity_comment” field

AOP source: https://aopwiki.org/aops/433 Data source: https://www.ebi.ac.uk/chembl/ Data curation: 10.3389/fphar.2022.951083

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Author Edoardo Luca Viganò
Version 0.1
Last Updated October 25, 2024, 14:17 (UTC)
Created October 25, 2024, 14:15 (UTC)
Size 48929458