DOFETILIDE BDBM50031720 N-[4-(2-{[2-(4-Methanesulfonylamino-phenyl)-ethyl]-methyl-amino}-ethoxy)-phenyl]-methanesulfonamide (UK-68798) N-[4-(2-{[2-(4-methanesulfonylamino-phenoxy)-ethyl]-methyl-amino}-ethyl)-phenyl]-methanesulfonamide UK-68,798 N-[4-(2-{[2-(4-METHANESULFONYLAMINO-PHENYL)-ETHYL]-METHYL-AMINO}-ETHOXY)-PHENYL]-METHANESULFONAMIDE DOFETILIDE (Dofetilide) N-[4-(2-{[2-(4-Methanesulfonylamino-phenyl)-ethyl]-methylamino}-ethoxy)-phenyl]-methanesulfonamide N-[4-(2-{[2-(4-Methanesulfonylamino-phenyl)-ethyl]-methyl-amino}-ethoxy)-phenyl]-methanesulfonamide (dofetilide) TIKOSYN US10167299, Dofetilide CHEMBL473
- Carvalho, JF; Louvel, J; Doornbos, ML; Klaasse, E; Yu, Z; Brussee, J; IJzerman, AP Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide. J Med Chem 56: 2828-40 (2013)
- Singleton, DH; Boyd, H; Steidl-Nichols, JV; Deacon, M; Groot, MJ; Price, D; Nettleton, DO; Wallace, NK; Troutman, MD; Williams, C; Boyd, JG Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. J Med Chem 50: 2931-41 (2007)
- ChEMBL_458742 (CHEMBL943026) Displacement of dofetilide from hERG
- ChEMBL_1496195 (CHEMBL3579079) Inhibition of dofetilide binding to human ERG
- ChEMBL_1512016 (CHEMBL3610728) Inhibition of dofetilide binding to human ERG
- ChEMBL_1566930 (CHEMBL3790710) Inhibition of dofetilide binding to human ERG
- ChEMBL_1663619 (CHEMBL4013300) Inhibition of dofetilide binding to human ERG
- ChEMBL_1689733 (CHEMBL4040303) Inhibition of dofetilide binding to human ERG
- ChEMBL_2027231 (CHEMBL4681389) Inhibition of dofetilide binding to human ERG
- ChEMBL_2266263 Displacement of [3H]-dofetilide from human ERG
- ChEMBL_408752 (CHEMBL909940) Displacement of [3H]dofetilide from hERG
- ChEMBL_593412 (CHEMBL1040540) Displacement of dofetilide from human ERG
- ChEMBL_625166 (CHEMBL1115187) Displacement of dofetilide from human ERG
- ChEMBL_629418 (CHEMBL1105771) Displacement of labeled dofetilide human ERG
- ChEMBL_727753 (CHEMBL1686112) Displacement of dofetilide from human ERG
- ChEMBL_741669 (CHEMBL1769661) Displacement of labeled dofetilide human ERG
- ChEMBL_797977 (CHEMBL1942854) Displacement of dofetilide from human ERG
- ChEMBL_811993 (CHEMBL2013363) Displacement of dofetilide from human ERG
- ChEMBL_812135 (CHEMBL2013639) Displacement of dofetilide from human ERG
- ChEMBL_812892 (CHEMBL2020267) Displacement of dofetilide from human ERG
- ChEMBL_821302 (CHEMBL2040132) Displacement of dofetilide from human ERG
- ChEMBL_878181 (CHEMBL2184102) Displacement of dofetilide from human ERG
- ChEMBL_1464651 (CHEMBL3406672) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_1543914 (CHEMBL3749896) Displacement of dofetilide from human ERG channel
- ChEMBL_1570047 (CHEMBL3789410) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_1680433 (CHEMBL4030710) Displacement of 3H-dofetilide from human ERG
- ChEMBL_1794818 (CHEMBL4266935) Displacement of 3H-dofetilide from human ERG
- ChEMBL_2051270 (CHEMBL4705969) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_2061618 (CHEMBL4716871) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_2151772 (CHEMBL5036234) Displacement of [3H]-dofetilide from human ERG
- ChEMBL_465006 (CHEMBL948183) Displacement of [3H]Dofetilide from human ERG
- ChEMBL_514034 (CHEMBL976349) Displacement of radiolabeled dofetilide from human ERG
- ChEMBL_581596 (CHEMBL1062483) Displacement of [3H]dofetilide from human ERG
- ChEMBL_598590 (CHEMBL1044431) Displacement of [3H]dofetilide from human ERG
- ChEMBL_624296 (CHEMBL1106981) Displacement of [3H]Dofetilide from human ERG
- ChEMBL_634882 (CHEMBL1120514) Displacement of [3H]dofetilide from human ERG
- ChEMBL_664671 (CHEMBL1260557) Displacement of [3H]dofetilide from human ERG
- ChEMBL_675694 (CHEMBL1274055) Displacement of [3H]dofetilide from human ERG
- ChEMBL_687158 (CHEMBL1291783) Displacement of [3H]-dofetilide from human hERG
- ChEMBL_687332 (CHEMBL1292008) Displacement of [3H]-dofetilide from human ERG
- ChEMBL_700297 (CHEMBL1647515) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_700343 (CHEMBL1647669) Displacement of [3H]dofetilide from human ERG
- ChEMBL_716659 (CHEMBL1670484) Displacement of [3H]-dofetilide from human ERG
- ChEMBL_750496 (CHEMBL1786160) Displacement of labeled dofetilide from human ERG
- ChEMBL_759400 (CHEMBL1810638) Displacement of labeled-dofetilide from human ERG
- ChEMBL_801017 (CHEMBL1948791) Displacement of [3H]dofetilide from human ERG
- ChEMBL_803863 (CHEMBL1954401) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_813365 (CHEMBL2019592) Displacement of [3H]dofetilide from human ERG
- ChEMBL_819957 (CHEMBL2032544) Displacement of [3H]dofetilide from human ERG
- ChEMBL_822867 (CHEMBL2037899) Displacement of [3H]dofetilide from human ERG
- ChEMBL_848013 (CHEMBL2150564) Displacement of [3H]dofetilide from human ERG
- ChEMBL_856088 (CHEMBL2162322) Displacement of [3H]-dofetilide from human ERG
- ChEMBL_879196 (CHEMBL2208509) Displacement of [3H]dofetilide from human ERG
- ChEMBL_941692 (CHEMBL2330862) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_948313 (CHEMBL2340694) Inhibition of human ERG by dofetilide binding assay
- ChEMBL_1339147 (CHEMBL3243282) Binding affinity to human ERG by dofetilide binding assay
- ChEMBL_1445007 (CHEMBL3372415) Inhibition of human ERG channel by dofetilide binding assay
- ChEMBL_1857771 (CHEMBL4358500) Inhibition of dofetilide binding to flag-tagged human ERG
- ChEMBL_1930023 (CHEMBL4433274) Displacement of [3H]Dofetilide from human ERG human
- ChEMBL_2295216 Inhibition of recombinant hERG in the presence of dofetilide by competitive binding assay
- ChEMBL_368880 (CHEMBL865554) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_473957 (CHEMBL950337) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_490851 (CHEMBL993590) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_498652 (CHEMBL967818) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_514608 (CHEMBL979986) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_515691 (CHEMBL993079) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_558175 (CHEMBL962309) Displacement of [3H]dofetilide from human ERG channel
- ChEMBL_689721 (CHEMBL1635449) Displacement of [3H]dofetilide from human ERG by SPA
- ChEMBL_1714634 (CHEMBL4124683) Inhibition of dofetilide binding to human ERG by fluorescence polarization assay
- ChEMBL_1783529 (CHEMBL4255046) Inhibition of human ERG by [3H]dofetilide binding displacement assay
- ChEMBL_351827 (CHEMBL870781) Displacement of [3H]dofetilide from hERG expressed in HEK293 cells
- ChEMBL_434539 (CHEMBL914755) Displacement of [3H]dofetilide from hERG expressed in HEK293 cells
- ChEMBL_446344 (CHEMBL895464) Displacement of [3H]dofetilide from hERG expressed in CHO cells
- ChEMBL_454647 (CHEMBL886667) Displacement of [3H]dofetilide from hERG expressed in HEK cells
- ChEMBL_501246 (CHEMBL976148) Displacement of [3H]dofetilide human ERG expressed in CHO cells
- ChEMBL_535682 (CHEMBL988836) Displacement of [3H]dofetilide from human ERG in HEK293 cells
- ChEMBL_649965 (CHEMBL1219663) Displacement of [3H]dofetilide from human ERG at 10 uM
- ChEMBL_686321 (CHEMBL1293077) Displacement of [3H]-dofetilide in human ERG expressed in CHO cells
- ChEMBL_875808 (CHEMBL2186754) Displacement of [3H]dofetilide to human ERG expressed in HEK293 cells
- ChEMBL_886196 (CHEMBL2210904) Inhibition of dofetilide binding to human ERG by patch clamp assay
- ChEMBL_1455308 (CHEMBL3362672) Inhibition of human ERG expressed in CHO cells by dofetilide binding assay
- ChEMBL_1461648 (CHEMBL3395117) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_1622464 (CHEMBL3864816) Inhibition of radiolabeled dofetilide binding to human ERG expressed in HEK293 cells
- ChEMBL_1703524 (CHEMBL4054757) Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cells
- ChEMBL_1765499 (CHEMBL4200746) Displacement of [3H]dofetilide from human ERG by high throughput assay
- ChEMBL_1829703 (CHEMBL4329577) Binding affinity to human ERG by dofetilide fluorescence polarization binding assay
- ChEMBL_2067975 (CHEMBL4723228) Inhibition of human ERG channel in presence of dofetilide by competition binding assay
- ChEMBL_2094125 (CHEMBL4775388) Binding affinity to human ERG by dofetilide fluorescence polarization binding assay
- ChEMBL_420606 (CHEMBL854891) Displacement of 3H-dofetilide from hERG-expressing HEK membrane homogenates
- ChEMBL_421696 (CHEMBL854890) Displacement of 3H-dofetilide from hERG-expressing HEK membrane homogenates
- ChEMBL_438371 (CHEMBL886338) Displacement of [3H]dofetilide from human ERG by fliter binding assay
- ChEMBL_438965 (CHEMBL889315) Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA
- ChEMBL_449357 (CHEMBL899624) Displacement of [3H]dofetilide from human HERG expressed in HEK293 cells
- ChEMBL_454875 (CHEMBL886903) Displacement of [3H]dofetilide from hERG expressed in HEK293 cell membrane
- ChEMBL_540897 (CHEMBL1026571) Displacement of [3H]dofetilide form human ERG expressed in HEK239 cells
- ChEMBL_541084 (CHEMBL1034067) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_543516 (CHEMBL1019465) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_544232 (CHEMBL1009827) Displacement of [3H]dofetilide from human ERG receptor by FLIPR method
- ChEMBL_564830 (CHEMBL954296) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_596933 (CHEMBL1048874) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_597420 (CHEMBL1039906) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_612185 (CHEMBL1074123) Displacement of radiolabeled dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_614260 (CHEMBL1106923) Displacement of [3H]dofetilide from human ERG by scintillation proximity assay
- ChEMBL_617393 (CHEMBL1101904) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_622966 (CHEMBL1112218) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_634306 (CHEMBL1120719) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_645081 (CHEMBL1211587) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_657972 (CHEMBL1248651) Displacement of [3H]-dofetilide from human ERG by scintillation proximity assay
- ChEMBL_665566 (CHEMBL1261450) Displacement of [3H]-dofetilide from human ERG by scintillation proximity assay
- ChEMBL_685210 (CHEMBL1287098) Displacement of [3H]dofetilide from human ERG by scintillation proximity assay
- ChEMBL_702661 (CHEMBL1657597) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_739892 (CHEMBL1762952) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_746773 (CHEMBL1776942) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_793275 (CHEMBL1931724) Displacement of [3H]dofetilide from human ERG by liquid scintillation counting
- ChEMBL_804055 (CHEMBL1952450) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_849758 (CHEMBL2150540) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
- ChEMBL_1442553 (CHEMBL3372246) Inhibition of human ERG expressing HEK293 cells by [3H]dofetilide binding assay
- ChEMBL_1570074 (CHEMBL3789676) Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells
- ChEMBL_1629116 (CHEMBL3871742) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cell membranes
- ChEMBL_1693545 (CHEMBL4044435) Displacement of [3H]-dofetilide from recombinant human ERG expressed in HEK293 cells
- ChEMBL_454227 (CHEMBL903410) Displacement of [3H]dofetilide from human ERG channel expressed in HEK293 cells
- ChEMBL_461984 (CHEMBL944827) Displacement of [3H]dofetilide from human ERG channel expressed in HEK293 cells
- ChEMBL_462632 (CHEMBL928561) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes
- ChEMBL_556966 (CHEMBL958152) Displacement of [3H]dofetilide from human recombinant ERG expressed in HEK293 cells
- ChEMBL_577524 (CHEMBL1057876) Displacement of [3H]dofetilide from human ERG channel by scintillation proximity assay
- ChEMBL_582205 (CHEMBL1059865) Displacement of [3H]dofetilide from human ERG channel by scintillation proximity assay
- ChEMBL_633902 (CHEMBL1120468) Displacement of [3H]-dofetilide from human ERG receptor expressed HEK cells
- ChEMBL_673956 (CHEMBL1275133) Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cells
- ChEMBL_686392 (CHEMBL1293148) Displacement of [3H]-dofetilide in human ERG expressed in CHO cells by proximity assay
- ChEMBL_746943 (CHEMBL1777309) Displacement of [3H]dofetilide from human ERG channel expressed in HEK293 cells
- ChEMBL_766668 (CHEMBL1827362) Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay
- ChEMBL_828971 (CHEMBL2060621) Displacement of [3H]dofetilide from human Erg expressed in human HEK293 cells
- ChEMBL_1554003 (CHEMBL3768210) Displacement of [3H]-dofetilide from human ERG potassium channel by scintillation proximity assay
- ChEMBL_424194 (CHEMBL907268) Displacement of [3H]dofetilide from human ERG potassium channel expressed in HEK293 cells
- ChEMBL_727759 (CHEMBL1686118) Displacement of [3H]Dofetilide from human CRTH2 receptor expressed in HEK293 cell membranes
- ChEMBL_772911 (CHEMBL1838314) Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 by scintillation counting
- ChEMBL_1448459 (CHEMBL3378079) Inhibition of human ERG over-expressed in HEK293 cell membrane by [3H]dofetilide binding assay
- ChEMBL_1729718 (CHEMBL4144996) Displacement of fluorescent-labelled dofetilide from human ERG expressed in HEK293 cell membrane homogenates
- ChEMBL_2100973 (CHEMBL4809369) Displacement of [3H]-dofetilide from human ERG after 60 mins by scintillation counting method
- ChEMBL_624022 (CHEMBL1116908) Displacement of [3H]dofetilide from human ERG expressed in CHO cells by patch clamp method
- ChEMBL_2079116 (CHEMBL4734907) Displacement of [3H]dofetilide from human ERG stably expressed in HEK293 cell membranes assessed as unlabelled dofetilide IC50 at 10 uM measured after 60 mins by microbeta liquid scintillation counting method (Rvb = 9.1 to 11.7 nM)
- ChEMBL_2079117 (CHEMBL4734908) Displacement of [3H]dofetilide from human ERG stably expressed in HEK293 cell membranes assessed as unlabelled dofetilide IC50 at 3 uM measured after 60 mins by microbeta liquid scintillation counting method (Rvb = 9.1 to 11.7 nM)
- ChEMBL_2079118 (CHEMBL4734909) Displacement of [3H]dofetilide from human ERG stably expressed in HEK293 cell membranes assessed as unlabelled dofetilide IC50 at 1 uM measured after 60 mins by microbeta liquid scintillation counting method (Rvb = 9.1 to 11.7 nM)
- ChEMBL_2079119 (CHEMBL4734910) Displacement of [3H]dofetilide from human ERG stably expressed in HEK293 cell membranes assessed as unlabelled dofetilide IC50 at 0.5 uM measured after 60 mins by microbeta liquid scintillation counting method (Rvb = 9.1 to 11.7 nM)
- ChEMBL_1745406 (CHEMBL4179916) Displacement of [3H]Dofetilide from recombinant human ERG after 60 mins by scintillation counting method
- ChEMBL_1811484 (CHEMBL4310944) Displacement of [3H]dofetilide from recombinant human ERG after 60 mins by scintillation counting method
- ChEMBL_1864061 (CHEMBL4365036) Displacement of [3H]dofetilide from recombinant human ERG after 60 mins by scintillation counting analysis
- ChEMBL_1881829 (CHEMBL4383328) Displacement of [3H]-Dofetilide from recombinant human ERG after 60 mins by scintillation counting analysis
- ChEMBL_1930021 (CHEMBL4433272) Displacement of [3H]Dofetilide from human ERG human expressed in HEK293 cells incubated for 45 mins
- ChEMBL_594120 (CHEMBL1036929) Displacement of [3H]dofetilide from human recombinant ERG expressed in HEK293 cells by patch clamp method
- ChEMBL_772749 (CHEMBL1837361) Displacement of [3H]dofetilide from human ERG transfected in HEK293 cells by fluorescence polarization binding assay
- ChEMBL_815080 (CHEMBL2024805) Displacement of [3H]Dofetilide from human ERG expressed in CHO-K1 cells by scintillation proximity assay
- ChEMBL_815356 (CHEMBL2026860) Displacement of [3H]Dofetilide from human ERG expressed in CHO-K1 cells by scintillation proximity assay
- ChEMBL_1504608 (CHEMBL3591513) Displacement of [3H]dofetilide from human Kv11.1 expressed in HEK293 cell membranes by competitive radioligand displacement assay
- ChEMBL_158556 (CHEMBL768699) Displacement of [3H]dofetilide from HEK cells expressing hERG voltage dependent IKr potassium channel Kv11.1
- ChEMBL_1751570 (CHEMBL4186330) Displacement of [3H]Dofetilide from human ERG expressed in HEK293 cells after 60 mins by scintillation spectrometry
- ChEMBL_1985231 (CHEMBL4618637) Displacement of [3H]dofetilide from recombinant human ERG measured after 60 mins by scintillation counting method
- ChEMBL_214800 (CHEMBL816205) Displacement of [3H]-dofetilide to HEK cells stably expressing hERG voltage-gated IKr potassium channel Kv11.1
- ChEMBL_1622890 (CHEMBL3865242) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cell membranes after 90 mins by scintillation counting
- ChEMBL_1677359 (CHEMBL4027502) Displacement of [3H]Dofetilide from human ERG expressed in HEK cells after 180 mins by scintillation counting method
- ChEMBL_1713877 (CHEMBL4123926) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 45 mins by scintillation counting method
- ChEMBL_1925813 (CHEMBL4428885) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 45 mins by scintillation counting analysis
- ChEMBL_465784 (CHEMBL948146) Displacement of [3H]dofetilide from human recombinant ERG potassium channel expressed in HEK293 cells by patch clamp method
- ChEMBL_714615 (CHEMBL1663293) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 60 mins by liquid scintillation counting
- ChEMBL_741328 (CHEMBL1764797) Displacement of [3H]-dofetilide from human ERG expressed in human HEK293 cells after 90 mins by scintillation counting
- ChEBML_1567397 Displacement of [3H]dofetilide from human ERG channel expressed in HEK293 cells after 60 mins by liquid scintillation counting method
- ChEMBL_1452204 (CHEMBL3365826) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes incubated for 90 mins by beta-counting method
- ChEMBL_1628382 (CHEMBL3870967) Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assay
- ChEMBL_1789191 (CHEMBL4260925) Displacement of [3H]-dofetilide from human ERG expressed in CHO cell membranes after 90 mins by micro-beta counting
- ChEMBL_1800357 (CHEMBL4272649) Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
- ChEMBL_1804555 (CHEMBL4303779) hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells
- ChEMBL_1924853 (CHEMBL4427809) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cells measured after 90 mins by scintillation proximity assay
- ChEMBL_1926979 (CHEMBL4430051) Displacement of [3H]dofetilide from recombinant human ERG transfected in HEK293 cell membranes after 60 mins by scintillation counting
- ChEMBL_1929870 (CHEMBL4433046) Inhibition of human ERG expressed in CHOK1 cell membranes after 2 hrs by cy3b-dofetilide-based fluorescence polarization assay
- ChEMBL_1972154 (CHEMBL4604972) Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
- ChEMBL_1973040 (CHEMBL4605858) Displacement of [3H]-dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
- ChEMBL_772880 (CHEMBL1838283) Inhibition of human ERG expressed in CHO-K1 cells after 2 hrs by Cy3b-Dofetilide-based fluorescence polarisation assay
- ChEMBL_815278 (CHEMBL2026493) Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cells after 45 mins by scintillation counting method
- ChEMBL_1462014 (CHEMBL3396464) Displacement of [3H]-dofetilide from human ERG expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
- ChEMBL_1504611 (CHEMBL3591516) Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as binding affinity constant by [3H]dofetilide competition association assay
- ChEMBL_1567397 (CHEMBL3789775) Displacement of [3H]dofetilide from human ERG channel expressed in HEK293 cells after 60 mins by liquid scintillation counting method
- ChEMBL_1577772 (CHEMBL3807756) Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting analysis
- ChEMBL_1929293 (CHEMBL4432469) Inhibition of [3H]dofetilide binding to human ERG expressed in HEK293 cell membranes after 60 mins by liquid scintillation spectrometric analysis
- ChEMBL_2125084 (CHEMBL4834317) Displacement of [3H]-dofetilide from human ERG expressed in CHO cell after 90 mins by microbeta liquid scintillation counting method
- ChEMBL_1441679 (CHEMBL3377656) Inhibition of human ERG channel expressed in HEK293 cells assessed as [3H]-dofetilide binding after 90 mins by liquid scintillation counting analysis
- ChEMBL_1540367 (CHEMBL3742791) Induction of dissociation of [3H]-dofetilide from Kv11.1 channel (unknown origin) assessed as dissociation rate expressed in HEK293 cells after 1 hr
- ChEMBL_1623007 (CHEMBL3865359) Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method
- ChEMBL_1744232 (CHEMBL4178742) Displacement of [3H]dofetilide from recombinant human ERG expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
- ChEMBL_1839450 (CHEMBL4339665) Displacement of [3H]dofetilide from recombinant human ERG expressed in HEK293 cell membranes measured after 80 mins by TopCount scintillation analysis
- ChEMBL_1910901 (CHEMBL4413347) Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting method
- ChEMBL_1696845 (CHEMBL4047735) Displacement of [3H]-Dofetilide from recombinant human ERG expressed in CHOK1 cell membranes incubated for 4 hrs under dark condition by luminescence assay
- ChEMBL_2204131 (CHEMBL5116839) Displacement of [3H]dofetilide from recombinant human ERG stably expressed in HEK293 cell membranes measured after 60 mins by scintillation counting analysis
- ChEMBL_2079104 (CHEMBL4734895) Displacement of [3H]dofetilide from human ERG stably expressed in HEK293 cell membranes measured after 60 mins by microbeta liquid scintillation counting method
- ChEMBL_2125318 (CHEMBL4834663) Displacement of [3H]dofetilide from recombinant human ERG stably expressed in HEK293 cell membranes measured after 90 mins by microbeta liquid scintillation counting method
- Inhibition of Specific Binding to the hERG-Receptor (HERGBD) After thawing on the day of the assay, the membrane suspension was diluted further with 20 mM HEPES/0.1 mM KCl/pH 7.2.The incubation mixture of 200 μl contained 1.5 nmol/l 3H-Dofetilide, optimized amount of membrane preparation, 20 mM HEPES/0.1 mM KCl/(pH 7.2) and inhibitor in 1% DMSO. Nonspecific binding was estimated in the presence of 10 M Dofetilide. The samples were incubated for 90 min. at RT.Binding was terminated by filtration of the incubated membrane preparations using Filtermat B (Pharmacia, Uppsala Sweden) and a Micro Cell Harvester (Skatron, Lier, Norway). The Filtermat B had been presoaked with 1% polyethylen imine and carefully washed with 0.05 M Tris/HCl-buffer pH=7.7 after the filtration to separate free and bound radioactivity. The filters were counted in a scintillation counter (Betaplate 1205, Berthold, Wildbad, Germany) in order to determine the specific binding of [3H]-Dofetilide.
- Inhibition Assay Cells were split 2-3 times weekly between 1:3 and 1:4. For binding assays and membrane preparations the cell culture medium was removed, cells were washed with PBS. Crude membranes for radioligand binding experiments were prepared by scraping the cells off the dishes in ice cold 20 mM HEPES/0.1 mM KCl/pH 7.2. The cell suspension was homogenized on ice (Ultra turrax, 3×20 sec.) and the homogenate was spun for 10 min (1° C., 1000 g, OPTIMA, SW28, 2800 U/min). The supernatant was than centrifuged for 40 min at 100000 g (1° C., OPTIMA, SW28, 23000 U/min). The membrane pellet was resuspended in 20 mM HEPES/0.1 mM KCl/pH 7.2, frozen and stored at −80° C.After thawing on the day of the assay, the membrane suspension was diluted further with 20 mM HEPES/0.1 mM KCl/pH 7.2.The incubation mixture of 200 μl contained 1.5 nmol/l 3H-Dofetilide, optimized amount of membrane preparation, 20 mM HEPES/0.1 mM KCl/(pH 7.2) and inhibitor in 1% DMSO. Nonspecific binding was estimated in the presence of 10 M Dofetilide. The samples were incubated for 90 min. at RT.Binding was terminated by filtration of the incubated membrane preparations using Filtermat B (Pharmacia, Uppsala Sweden) and a Micro Cell Harvester (Skatron, Lier, Norway). The Filtermat B had been presoaked with 1% polyethylenimine and carefully washed with 0.05 M Tris/HCl-buffer pH=7.7 after the filtration to separate free and bound radioactivity. The filters were counted in a scintillation counter (Betaplate 1205, Berthold, Wildbad, Germany) in order to determine the specific binding of [3H]-Dofetilide.
- In Vitro Binding Assay Compounds were evaluated for binding to the human ether-a-go-go potassium channel (hERG) expressed in HEK293 cells by displacement of 3[H]-astemizole according to the methods by Finlayson et al. (K. Finlayson., L. Turnbull, C. T. January, J. Sharkey, J. S. Kelly; [3H]Dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur. J. Pharmacol. 2001, 430, 147-148). Compounds were incubated at 1 or 10 μM final concentration, in duplicate, and the amount of displaced 3[H]-astemizole determined by liquid scintillation spectroscopy. In some cases, a seven concentration (each concentration in duplicate) displacement curve was generated to determine an IC50.
- Inhibition of Specific Binding to the hERG Receptor (HERGBD) Binding was terminated by filtration of the incubated membrane preparations using Filtermat B (Pharmacia, Uppsala Sweden) and a Micro Cell Harvester (Skatron, Lier, Norway). The Filtermat B had been presoaked with 1% polyethylen imine and carefully washed with 0.05 M Tris/HCl-buffer pH=7.7 after the filtration to separate free and bound radioactivity. The filters were counted in a scintillation counter (Betaplate 1205, Berthold, Wildbad, Germany) in order to determine the specific binding of [3H]-Dofetilide. The optimal amount of membrane preparation in the assay was determined and optimized for each membrane preparation separately in front of using the membranes in compound testing. Test compounds were either screened at 6 to 10 increasing concentrations for the determination of IC50 and Ki or at 2-4 concentrations for the determination of the percent inhibition. For pipetting of the incubation mixture we routinely use the robot Biomek2000 (Fa. Beckman).