@article{APS9490,
author = {Hai-bo YU and Bei-yan ZOU and Xiao-liang WANG and Min LI},
title = {Investigation of miscellaneous hERG inhibition in large diverse compound collection using automated patch-clamp assay},
journal = {Acta Pharmacologica Sinica},
volume = {37},
number = {1},
year = {2017},
keywords = {},
abstract = {Aim: hERG potassium channels display miscellaneous interactions with diverse chemical scaffolds. In this study we assessed the hERG inhibition in a large compound library of diverse chemical entities and provided data for better understanding of the mechanisms underlying promiscuity of hERG inhibition.
Methods: Approximately 300 000 compounds contained in Molecular Library Small Molecular Repository (MLSMR) library were tested. Compound profiling was conducted on hERG-CHO cells using the automated patch-clamp platform–IonWorks QuattroTM.
Results: The compound library was tested at 1 and 10 μmol/L. IC50 values were predicted using a modified 4-parameter logistic model. Inhibitor hits were binned into three groups based on their potency: high (IC50},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/9490}
}