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Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists |
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| Authors: | Zhang Xuqing Hufnagel Heather Markotan Thomas Lanter James Cai Chaozhong Hou Cuifen Singer Monica Opas Evan McKenney Sandra Crysler Carl Johnson Dana Sui Zhihua |
| Institution: | Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States. xzhang5@prdus.jnj.com |
| Abstract: | A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG. |
| Keywords: | CCR2 hERG Azetidine |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |