title: Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists.
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.
authors.affiliation: Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States. xzhang5@prdus.jnj.com
authors.forename: Xuqing
authors.initials: X
authors.lastname: Zhang
authors.forename: Heather
authors.initials: H
authors.lastname: Hufnagel
authors.forename: Thomas
authors.initials: T
authors.lastname: Markotan
authors.forename: James
authors.initials: J
authors.lastname: Lanter
authors.forename: Chaozhong
authors.initials: C
authors.lastname: Cai
authors.forename: Cuifen
authors.initials: C
authors.lastname: Hou
authors.forename: Monica
authors.initials: M
authors.lastname: Singer
authors.forename: Evan
authors.initials: E
authors.lastname: Opas
authors.forename: Sandra
authors.initials: S
authors.lastname: McKenney
authors.forename: Carl
authors.initials: C
authors.lastname: Crysler
authors.forename: Dana
authors.initials: D
authors.lastname: Johnson
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006626:Hippurates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001384:Azetidines; C515334:CCR2 protein, human; D051638:Ether-A-Go-Go Potassium Channels; D006626:Hippurates; D054390:Receptors, CCR2