IndraLab

Statements

reach
"Interestingly, WAY-123,398, which did not inhibit [3 H] dofetilide binding to whole HEK293 cells (Finlayson et al., 2001b), reduced [3 H] dofetilide binding to HERG membranes, although not completely."
11698075
reach
"In addition, [3 H] dofetilide binding to HERG membranes was also reduced in a concentration dependent manner by the antipsychotics pimozide (K i = 70.6 +/-11.8 nM, n H = 0.89 +/-0.12, n = 4) and halop[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11698075
reach
"Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes : involvement of S6 sites."
10648647
reach
"Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a new benzthiazole series was designed, congeners of 1-3, which led to compounds 7a, 7c, 12a-d which exhibited LTA (4) H IC (50) = 3-6 nM and hERG Dofetilide Binding IC (50) = 8.9->> 10 muM."
23127888
reach
"[3H] dofetilide binding to HERG transfected membranes : a potential high throughput preclinical screen."
11698075
reach
"[3 H] dofetilide binding to HERG transfected membranes was performed in a sodium buffer without bovine serum albumin, as for whole cell studies (Finlayson et al., 2001b)."
11698075
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"In this study, we show that [3 H] dofetilide binding to HERG transfected membranes is inhibited by antiarrhythmics and structurally unrelated compounds known to prolong the QT interval in man.Human em[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11698075
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"Also, GZ-11610 inhibited [3 H] dofetilide binding to hERG channels expressed on HEK-293 cell membranes, with a Ki of 9.50 muM and an Imax of> 80% (XREF_FIG)."
29427069
reach
"Evaluation of GZ-793A for potential cardiac liabilities revealed that GZ-793A inhibited with high affinity (IC 50 = 0.81 +/- 0.11 muM) [3 H] dofetilide binding to hERG channels expressed by HEK-293 cells (XREF_FIG)."
27986625
reach
"Similar to female predominance of arrhythmia in the acquired setting, which suggests interactions between hERG, dofetilide and oestradiol, the female predominance of inherited arrhythmia linked the the G604S mutations, suggests that oestradiol may differentially interact with the mutant hERG channel compared to WT."
28516454
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"High-affinity dofetilide binding to hERG expressed in Xenopus oocytes involves Phe656 residue."
26543354
reach
"GZ-11610-induced inhibition of [3 H] dofetilide binding to hERG channels assessed potential cardiotoxicity."
29427069
reach
"The method for determining [3 H] dofetilide binding to hERG protein expressed by the cell membranes was described previously."
29427069