Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists

DOI: 10.1016/j.bmcl.2011.06.080

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 5577 - 5582 (2011)

Update date:2022-08-04

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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

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Article abstract of DOI:10.1016/j.bmcl.2011.06.080

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.

Full text of DOI:10.1016/j.bmcl.2011.06.080

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