IndraLab

Statements

reach
"However, the drug inhibition mechanism remains unclear because of the scarce structural information regarding the drug- and potassium bound hERG channels."
33450182
reach
"Design and SAR of the analogs for reducing hERG (human ether-a-go-go related gene) potassium ion channel binding affinity were also investigated in vitro as a safe-drug study."
27043173
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"Overall, i) several structures were found to be effectual for reducing hERG potassium ion channel binding affinity in this study."
27043173
reach
"Thus, 1 demonstrates dose-dependent inhibitory effect against mechanical allodynia in chronic constriction injury-induced neuropathic pain model rats, robust metabolic stability and little hERG potassium ion channel binding affinity, with its unique and potentially safe profiles and mechanisms, which were distinctive from those of N/OFQ in terms of site-differential effects."
20875743
reach
"The structure activity relationship (SAR) of the potency and selectivity, structure-metabolic stability relationship (SMR), and SAR of hERG (human ether-a-go-go related gene) potassium ion channel binding affinity for the analogs in the present studies invitro provided or suggested significant and/or useful structural determinants and insights for the respective purposes."
27043173
reach
"In this study, we obtained the cryo-EM density map of potassium bound hERG channel complexed with astemizole, a well-known hERG inhibitor that increases risk of potentially fatal arrhythmia, at 3.5-A resolution."
33450182