title: Discovery of thienopyridines as Src-family selective Lck inhibitors.
abstract: We describe the identification, SAR, and in vivo pharmacology of a new series of Src-family selective Lck inhibitors. These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck.
authors.affiliation: Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA.
authors.forename: Lily
authors.initials: L
authors.lastname: Abbott
authors.forename: Patrick
authors.initials: P
authors.lastname: Betschmann
authors.forename: Andrew
authors.initials: A
authors.lastname: Burchat
authors.forename: David J
authors.initials: DJ
authors.lastname: Calderwood
authors.forename: Heather
authors.initials: H
authors.lastname: Davis
authors.forename: Peter
authors.initials: P
authors.lastname: Hrnciar
authors.forename: Gavin C
authors.initials: GC
authors.lastname: Hirst
authors.forename: Biqin
authors.initials: B
authors.lastname: Li
authors.forename: Michael
authors.initials: M
authors.lastname: Morytko
authors.forename: Kelly
authors.initials: K
authors.lastname: Mullen
authors.forename: Bryant
authors.initials: B
authors.lastname: Yang
mesh_terms: D001665:Binding Sites; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors
chemical_list: D011725:Pyridines; C446540:thienopyridine; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck); D019061:src-Family Kinases