IndraLab

Statements

KCNH2 inhibits ion channel. 7 / 7
| 5 2
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"Prolongation of the QT interval, caused by many drugs beyond cardiac treatments, often arises from unintended ion channel blockades such as the hERG potassium channel, crucial for cardiac repolarization."
39725693
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"These include off-target pharmacology, ion channel inhibition including hERG (human Ether-a-go-go-Related Gene), in vitro genotoxicity including Ames and micronucleus tests, and phototoxicity studies."
30526594
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"To date, these formats have largely been used by pharmaceutical companies to screen for human ether-a-gogo-related gene (hERG) induced cardiac ion channel blockade (Möller and Witchel, 2011)."
30544081
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"However, the hERG test, which blocked a single ion channel in non–human mammalian cells, reported that not all compounds showing strong hERG channel inhibition cause lethal arrythmias in humans."
35303744
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"TBAJ-876 ( xref ) was selected from this series to progress to pre-clinical development due to its lower lipophilicity, lower hERG ion channel inhibition, higher clearance and retention of BDQ’s potent activity against Mtb [ xref ]."
31835707
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"Several heterocycles as well as different amido substituents were screened for their antiviral activity, oral bioavailability, and low propensity towards hERG ion channel inhibition and interaction with a range of CYP enzymes."
| PMC
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"A detailed investigation of pharmacological effects in this unique 3D cardiac tissue showed not only changes in repolarization caused by cardiac ion channel blockers such as HERG channel but also changes in contractility mediated by multiple mechanisms of action."
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