Medicinal Chemistry of hERG Optimizations: Highlights and Hang-Ups

Abbott G. W., 1999, Cell, 97, 187, 10.1016/S0092-8674(00)80728-X

Fermini B., 2003, Nat. Rev. Drug Discovery, 2, 447, 10.1038/nrd1108

Keating M. T., 2001, Cell, 104, 580, 10.1016/S0092-8674(01)00243-4

Pearlstein R., 2003, J. Med. Chem., 46, 2022, 10.1021/jm0205651

Finlayson K., 2001, Eur. J. Pharmacol., 430, 148, 10.1016/S0014-2999(01)01362-0

Product is commercially available from Molecular Devices Inc., 2006, http://www.moleculardevices.com/pages/instruments/patchxpress.html (accessed

Valentin J.-P., 2004, J. Pharmacol. Toxicol. Methods, 49, 181

Gintant G. A., 2001, J. Cardiovasc. Pharmacol., 37, 618, 10.1097/00005344-200105000-00012

Carlsson L, 2006, J. Intern. Med., 259, 80, 10.1111/j.1365-2796.2005.01590.x

Yamamoto K., 2001, Toxicol. Sci., 60, 176, 10.1093/toxsci/60.1.165

Gras J., 1999, Drug Safety, 21, 44, 10.2165/00002018-199921001-00006

Vaz R. J., 2005, Prog. Med. Chem., 43, 18

Aronov A. M, 2005, Drug Discovery Today, 10, 155, 10.1016/S1359-6446(04)03278-7

Recanatini M., 2005, Med. Res. Rev., 25, 166, 10.1002/med.20019

Mitcheson J. S., 2000, Proc. Natl. Acad. Sci. U.S.A., 97, 12333, 10.1073/pnas.210244497

Fernandez D., 2004, J. Biol. Chem., 279, 10127

Mitcheson J. S., 2003, Curr. Opin. Drug Discovery Dev., 6, 674

Ishii K., 2001, FEBS Lett., 506, 195, 10.1016/S0014-5793(01)02902-7

Sánchez-Chapula J. A., 2002, J. Biol. Chem., 277, 23595, 10.1074/jbc.M200448200

Perry M., 2004, Mol. Pharmacol., 66, 249, 10.1124/mol.104.000117

Witchel H. J., 2004, Mol. Pharmacol., 66, 1212, 10.1124/mol.104.001743

Sanguinetti M. C., 2005, Trends Pharmacol. Sci., 26, 124, 10.1016/j.tips.2005.01.003

Pearlstein R. A., 2003, Bioorg. Med. Chem. Lett., 13, 1835, 10.1016/S0960-894X(03)00196-3

Rajamani R., 2005, Bioorg. Med. Chem. Lett., 15, 1741, 10.1016/j.bmcl.2005.01.008

Österberg F., 2005, FEBS Lett., 579, 2944, 10.1016/j.febslet.2005.04.039

Wood A., 2005, Prog. Med. Chem., 43, 271

Cavalli A., 2002, J. Med. Chem., 45, 3853

Ekins S., 2002, J. Pharmacol. Exp. Ther., 301, 434, 10.1124/jpet.301.2.427

Du L.-P., 2004, Bioorg. Med. Chem. Lett., 14, 4777

Cianchetta G., 2005, Bioorg. Med. Chem. Lett., 15, 3642, 10.1016/j.bmcl.2005.03.062

Keserü G. M, 2003, Bioorg. Med. Chem. Lett., 13, 2775, 10.1016/S0960-894X(03)00492-X

Bains W., 2004, Prog. Biophys. Mol. Biol., 86, 233, 10.1016/j.pbiomolbio.2003.09.001

Song M., 2006, J. Chem. Inf. Model., 46, 300, 10.1021/ci050308f

Zolotoy A. B., 2003, Physicochemical determinants for drug induced blockade of HERG potassium channels:  effect of charge and charge shielding. Curr. Med. Chem.:  Cardiovasc. Hematol. Agents

Roche O., 2002, ChemBioChem, 3, 459, 10.1002/1439-7633(20020503)3:5<455::AID-CBIC455>3.0.CO;2-L

O'Brien S. E., 2005, J. Med. Chem., 48, 1291, 10.1021/jm049254b

Tobita M., 2005, Bioorg. Med. Chem. Lett., 15, 2890, 10.1016/j.bmcl.2005.03.080

Buyck C., 2002, 14th European Symposium on Quantitative Structure−Activity Relationships

Aptula A. O., 2004, SAR QSAR Environ. Res., 15, 411, 10.1080/10629360412331297353

Aronov A. M., 2004, Bioorg. Med. Chem., 12, 2315, 10.1016/j.bmc.2004.02.003

Stouch T. R., 2003, In silico ADME/Tox:  why models fail. J. Comput.-Aided Mol. Des

version 4.10

Bell I. M., 2001, J. Med. Chem., 44, 2949

Bell I. M., 2002, J. Med. Chem., 45, 2409

Blum C. A., 2004, J. Med. Chem., 47, 2325

McCauley J. A., 2004, J. Med. Chem., 47, 2096, 10.1021/jm030483s

Kim D., 2005, Bioorg. Med. Chem. Lett., 15, 2134

Shu M., 2004, Bioorg. Med. Chem. Lett., 14, 952

Ahmad S., 2004, Bioorg. Med. Chem. Lett., 14, 102

Kang J., 2001, Mol. Pharmacol., 59, 126

Collins I., 1998, Bioorg. Med. Chem., 6, 753, 10.1016/S0968-0896(98)00028-5

Rowley M., 2001, J. Med. Chem., 44, 1614

Fish L. R., 2005, Bioorg. Med. Chem. Lett., 15, 3669

Woosley R. L, 1996, Annu. Rev. Pharmacol. Toxicol., 36, 252, 10.1146/annurev.pa.36.040196.001313

Rampe D., 1993, Mol. Pharmacol., 44, 1245

Xu J., 2005, Bioorg. Med. Chem. Lett., 15, 2536

Edmonson S. D., 2004, Bioorg. Med. Chem. Lett., 14, 5155

Edmondson S. D., 2005, Bioorg. Med. Chem. Lett., 15, 3052, 10.1016/j.bmcl.2005.04.028

Vaz R. J., 2004, Bioorg. Med. Chem. Lett., 14, 6056

Fraley M. E., 2004, Bioorg. Med. Chem. Lett., 14, 355, 10.1016/j.bmcl.2003.11.007

Fletcher S. R., 2002, J. Med. Chem., 45, 503, 10.1021/jm011030v

Cooper L. C., 2002, Bioorg. Med. Chem. Lett., 12, 1762

Friesen R. W., 2003, J. Med. Chem., 46, 2426, 10.1021/jm0204542

Bilodeau M. T., 2004, J. Med. Chem., 47, 6372, 10.1021/jm049697f

Matasi J. J., 2005, Bioorg. Med. Chem. Lett., 15, 3678

Zhang H. C., 2005, J. Med. Chem., 48, 1728

Bourrain S., 1998, Bioorg. Med. Chem., 6, 1743, 10.1016/S0968-0896(98)00134-5

Liang J., 2005, Bioorg. Med. Chem. Lett., 15, 2947

Long S. B., 2005, Science, 309, 903, 10.1126/science.1116270

Kang J., 2006, Anesthesiology, 104, 1022, 10.1097/00000542-200605000-00018

Kuryshev Y. A., 2005, J. Pharmacol. Exp. Ther., 312, 323, 10.1124/jpet.104.073692