Literature DB >> 16377185

Synthesis of the first sulfur-35-labeled hERG radioligand.

Conrad E Raab1, John W Butcher, Thomas M Connolly, Jerzy Karczewski, Nathan X Yu, Steven J Staskiewicz, Nigel Liverton, Dennis C Dean, David G Melillo.   

Abstract

The synthesis of the first high specific activity S-35-labeled hERG radioligand, [(35)S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [(35)S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.

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Year:  2006        PMID： 16377185     DOI： 10.1016/j.bmcl.2005.12.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Compilation and physicochemical classification analysis of a diverse hERG inhibition database.

Authors:  Remigijus Didziapetris; Kiril Lanevskij
Journal:  J Comput Aided Mol Des       Date:  2016-10-25       Impact factor: 3.686

2.  Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Authors:  Shuwen He; Qingmei Hong; Zhong Lai; David X Yang; Pauline C Ting; Jeffrey T Kuethe; Timothy A Cernak; Kevin D Dykstra; Donald M Sperbeck; Zhicai Wu; Yang Yu; Ginger X Yang; Tianying Jian; Jian Liu; Deodial Guiadeen; Arto D Krikorian; Lisa M Sonatore; Judyann Wiltsie; Jinqi Liu; Judith N Gorski; Christine C Chung; Jack T Gibson; JeanMarie Lisnock; Jianying Xiao; Michael Wolff; Sharon X Tong; Maria Madeira; Bindhu V Karanam; Dong-Ming Shen; James M Balkovec; Shirly Pinto; Ravi P Nargund; Robert J DeVita
Journal:  ACS Med Chem Lett       Date:  2014-09-08       Impact factor: 4.345

3.  Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

Authors:  Zhi-Qiang Yang; Kelly-Ann S Schlegel; Youheng Shu; Thomas S Reger; Rowena Cube; Christa Mattern; Paul J Coleman; Jim Small; George D Hartman; Jeanine Ballard; Cuyue Tang; Yuhsin Kuo; Thomayant Prueksaritanont; Cindy E Nuss; Scott Doran; Steve V Fox; Susan L Garson; Yuxing Li; Richard L Kraus; Victor N Uebele; Adekemi B Taylor; Wei Zeng; Wei Fang; Cynthia Chavez-Eng; Matthew D Troyer; Julie Ann Luk; Tine Laethem; William O Cook; John J Renger; James C Barrow
Journal:  ACS Med Chem Lett       Date:  2010-08-24       Impact factor: 4.345

4.  The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

Authors:  Shuwen He; Zhixiong Ye; Quang Truong; Shrenik Shah; Wu Du; Liangqin Guo; Peter H Dobbelaar; Zhong Lai; Jian Liu; Tianying Jian; Hongbo Qi; Raman K Bakshi; Qingmei Hong; James Dellureficio; Alexander Pasternak; Zhe Feng; Reynalda deJesus; Lihu Yang; Mikhail Reibarkh; Scott A Bradley; Mark A Holmes; Richard G Ball; Rebecca T Ruck; Mark A Huffman; Frederick Wong; Koppara Samuel; Vijay B Reddy; Stan Mitelman; Sharon X Tong; Gary G Chicchi; Kwei-Lan Tsao; Dorina Trusca; Margaret Wu; Qing Shao; Maria E Trujillo; George J Eiermann; Cai Li; Bei B Zhang; Andrew D Howard; Yun-Ping Zhou; Ravi P Nargund; William K Hagmann
Journal:  ACS Med Chem Lett       Date:  2012-05-07       Impact factor: 4.345

5.  Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.

Authors:  Shuwen He; Zhong Lai; Zhixiong Ye; Peter H Dobbelaar; Shrenik K Shah; Quang Truong; Wu Du; Liangqin Guo; Jian Liu; Tianying Jian; Hongbo Qi; Raman K Bakshi; Qingmei Hong; James Dellureficio; Mikhail Reibarkh; Koppara Samuel; Vijay B Reddy; Stan Mitelman; Sharon X Tong; Gary G Chicchi; Kwei-Lan Tsao; Dorina Trusca; Margaret Wu; Qing Shao; Maria E Trujillo; Guillermo Fernandez; Donald Nelson; Patricia Bunting; Janet Kerr; Patrick Fitzgerald; Pierre Morissette; Sylvia Volksdorf; George J Eiermann; Cai Li; Bei Zhang; Andrew D Howard; Yun-Ping Zhou; Ravi P Nargund; William K Hagmann
Journal:  ACS Med Chem Lett       Date:  2014-04-21       Impact factor: 4.345

6.  MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Authors:  Nigel J Liverton; Steven S Carroll; Jillian Dimuzio; Christine Fandozzi; Donald J Graham; Daria Hazuda; M Katherine Holloway; Steven W Ludmerer; John A McCauley; Charles J McIntyre; David B Olsen; Michael T Rudd; Mark Stahlhut; Joseph P Vacca
Journal:  Antimicrob Agents Chemother       Date:  2009-10-19       Impact factor: 5.191
  6 in total

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