IndraLab

Statements

KCNH2 inhibits IC 50. 3 / 3
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"Firstly, I Kr / hERG block aside, most of the IC 50 values from which the drug models were constructed were recorded from non human, mammalian species due to lack of human experimental data."
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"For example, Xing et al. reported that mutations at site 652 increased the blocking effect of capsaicin on hERG I kr current, decreasing the IC 50 to about one-fourth the value for the wild type chann[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Mutation of the phenylalanine amino acid residue at position 656 (F656) in the S6 region to either valine or alanine dramatically attenuates drug-mediated block of hERG, increasing the IC 50 for these[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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