Literature DB >> 16782336

Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc.

David A Price1, Duncan Armour, Marcel de Groot, Derek Leishman, Carolyn Napier, Manos Perros, Blanda L Stammen, Anthony Wood.   

Abstract

The discovery of maraviroc 17 is described with particular reference to the generation of high selectivity over affinity for the HERG potassium channel. This was achieved through the use of a high throughput binding assay for the HERG channel that is known to show an excellent correlation with functional effects.

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Year:  2006        PMID： 16782336     DOI： 10.1016/j.bmcl.2006.06.012

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


  9 in total

Review 1.  Chemokine receptor CCR5 antagonist maraviroc: medicinal chemistry and clinical applications.

Authors:  Guoyan G Xu; Jia Guo; Yuntao Wu
Journal:  Curr Top Med Chem       Date:  2014       Impact factor: 3.295

2.  ADMET evaluation in drug discovery. 12. Development of binary classification models for prediction of hERG potassium channel blockage.

Authors:  Sichao Wang; Youyong Li; Junmei Wang; Lei Chen; Liling Zhang; Huidong Yu; Tingjun Hou
Journal:  Mol Pharm       Date:  2012-03-16       Impact factor: 4.939

3.  Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.

Authors:  Mark D Andrews; Kerry Af Forselles; Kevin Beaumont; Sébastien R G Galan; Paul A Glossop; Mathilde Grenie; Alan Jessiman; Amy S Kenyon; Graham Lunn; Graham Maw; Robert M Owen; David C Pryde; Dannielle Roberts; Thien Duc Tran
Journal:  ACS Med Chem Lett       Date:  2015-01-30       Impact factor: 4.345

4.  Discovery of orally available spirodiketopiperazine-based CCR5 antagonists.

Authors:  Rena Nishizawa; Toshihiko Nishiyama; Katsuya Hisaichi; Keisuke Hirai; Hiromu Habashita; Yoshikazu Takaoka; Hideaki Tada; Kenji Sagawa; Shiro Shibayama; Kenji Maeda; Hiroaki Mitsuya; Hisao Nakai; Daikichi Fukushima; Masaaki Toda
Journal:  Bioorg Med Chem       Date:  2010-05-25       Impact factor: 3.641

5.  Investigation of mechanism of drug-induced cardiac injury and torsades de pointes in cynomolgus monkeys.

Authors:  D L Misner; C Frantz; L Guo; M R Gralinski; P B Senese; J Ly; M Albassam; K L Kolaja
Journal:  Br J Pharmacol       Date:  2012-04       Impact factor: 8.739

6.  Design and synthesis of a bivalent ligand to explore the putative heterodimerization of the mu opioid receptor and the chemokine receptor CCR5.

Authors:  Yunyun Yuan; Christopher K Arnatt; Guo Li; Kendra M Haney; Derong Ding; Joanna C Jacob; Dana E Selley; Yan Zhang
Journal:  Org Biomol Chem       Date:  2012-02-22       Impact factor: 3.876

7.  The N,N,O-Trisubstituted Hydroxylamine Isostere and Its Influence on Lipophilicity and Related Parameters.

Authors:  Jarvis Hill; David Crich
Journal:  ACS Med Chem Lett       Date:  2022-04-20       Impact factor: 4.632

Review 8.  HIV entry inhibitors and their potential in HIV therapy.

Authors:  Keduo Qian; Susan L Morris-Natschke; Kuo-Hsiung Lee
Journal:  Med Res Rev       Date:  2009-03       Impact factor: 12.944

9.  Discovery of HIV entry inhibitors via a hybrid CXCR4 and CCR5 receptor pharmacophore-based virtual screening approach.

Authors:  Muhammad Usman Mirza; Atefeh Saadabadi; Michiel Vanmeert; Outi M H Salo-Ahen; Iskandar Abdullah; Sandra Claes; Steven De Jonghe; Dominique Schols; Sarfraz Ahmad; Matheus Froeyen
Journal:  Eur J Pharm Sci       Date:  2020-09-02       Impact factor: 4.384
  9 in total

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