IndraLab

Statements

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"Mindful of this liability, we introduced the hERG dofetilide binding assay 7 early in our screening cascade."
21112782
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"Indeed, the binding of [ 3 H]dofetilide (a class III antiarrhythmic drug) to hERG channels has been previously characterized in cardiac myocytes (Chadwick et al., 1993; Duff, Feng, & Sheldon, 1995; Fi[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
15519905
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"The method for determining [3 H] dofetilide binding to hERG protein expressed by the cell membranes was described previously."
29427069
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"Molecular determinant of high affinity dofetilide binding to HERG1 expressed in Xenopus oocytes : involvement of S6 sites."
29697308
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"tatCN19o inhibition of [ H]dofetilide binding to hERG channel protein was used to assess its potential cardiotoxicity."
36747773
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"High-affinity dofetilide binding to hERG expressed in Xenopus oocytes involves Phe656 residue."
26543354
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"High-affinity dofetilide binding to hERG expressed in Xenopus Oocytes involves Phe656 residue (18)."
39386239
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"As is frequently observed, 8 we identified a positive correlation between c Log P and hERG dofetilide binding within the series and a negative correlation with polar surface area ( Fig. 3 )."
21112782
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"GZ-11610-induced inhibition of [3 H] dofetilide binding to hERG channels assessed potential cardiotoxicity."
29427069
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"When bound to the inactivated-state hERG model, dofetilide settles deeper into the pore, extending horizontally above the Y652 residue, where it forms π stacking and cation-π interactions, as well as hydrogen bonds with the Y652 residues of all subunits."
38352360
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"The compound showed weak activity in a hERG dofetilide binding assay (IC 50 13 μM)."
25754490
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"Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes : involvement of S6 sites."
10648647
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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
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"Radioactivity retained by the filters was determined as previously described.JPC-141 inhibition of [ 3 H]dofetilide binding to hERG channels was determined using previously described methods [53,42] ."
38580165
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"Locomotor activity was analyzed using a two-way mixed effects analysis, where treatment group (METH or saline) was a between-subjects factor and JPC-141 dose as a within-subjects factor, followed by w[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
38580165
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"[ 3 H]Dofetilide binding to hERG was inhibited by JPC-141 (Ki = 2.94 µM) and was 57-fold less potent at hERG than at VMAT2.When JPC-141 was administered either prior to or after the dose of METH which[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
38580165
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"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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"FINLAYSON K, TURNBULL L, JANUARY CT, SHARKEY J, KELLY JS : [3H] dofetilide binding to HERG transfected membranes : a potential high throughput preclinical screen."
17298291
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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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"[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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"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
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"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
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"tatCN19o inhibition of [ H]dofetilide binding to hERG channel protein was used to assess its potential cardiotoxicity."
37037305
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"As mentioned earlier 33b also showed significant affinity (pIC 50 7.1) for the hERG channel, having a similar potency to azelastine (pIC 50 = 7.0) in the hERG dofetilide binding assay."
28958623
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"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
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"For instance, ' false positive ' results obtained from the hERG dofetilide binding assay in comparison to the patch clamp negative data correlate well with low permeability observed in the Caco-2 and PAMPA assays."
17916053
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"LEES-MILLER JP, DUAN Y, TENG GQ, DUFF HJ : Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes : involvement of S6 sites."
17298291
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"This was evaluated by both patch clamp electrophysiology and inhibition of [ H]dofetilide binding to hERG channels over a range of TG11-77 concentrations."
36460083