title: Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.
abstract: Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are presented. Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors.
authors.affiliation: Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA. david.r.anderson@pfizer.com
authors.forename: David R
authors.initials: DR
authors.lastname: Anderson
authors.forename: Marvin J
authors.initials: MJ
authors.lastname: Meyers
authors.forename: Ravi G
authors.initials: RG
authors.lastname: Kurumbail
authors.forename: Nicole
authors.initials: N
authors.lastname: Caspers
authors.forename: Gennadiy I
authors.initials: GI
authors.lastname: Poda
authors.forename: Scott A
authors.initials: SA
authors.lastname: Long
authors.forename: Betsy S
authors.initials: BS
authors.lastname: Pierce
authors.forename: Matthew W
authors.initials: MW
authors.lastname: Mahoney
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Mourey
mesh_terms: D001665:Binding Sites; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D048370:MAP Kinase Kinase 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D047428:Protein Kinase Inhibitors; D013876:Thiophenes; C088015:benzothiophene; D051357:Cyclin-Dependent Kinase 2; D048370:MAP Kinase Kinase 2