title: N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.
abstract: Starting with a hit from vHTS attained by a docking procedure of virtual compounds into ATP pockets of different kinases applying the 4SCan technology, variations of the adenine mimic resulted in the identification of promising scaffolds, giving rise to in vitro IC(50) values in the nanomolar range on different kinases down to 63nM.
authors.affiliation: 4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Tasler
authors.forename: Oliver
authors.initials: O
authors.lastname: Müller
authors.forename: Tanja
authors.initials: T
authors.lastname: Wieber
authors.forename: Thomas
authors.initials: T
authors.lastname: Herz
authors.forename: Rolf
authors.initials: R
authors.lastname: Krauss
authors.forename: Frank
authors.initials: F
authors.lastname: Totzke
authors.forename: Michael H G
authors.initials: MH
authors.lastname: Kubbutat
authors.forename: Christoph
authors.initials: C
authors.lastname: Schächtele
mesh_terms: D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000378:metabolism; D001665:Binding Sites / Q000502:physiology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism
chemical_list: D052160:Benzothiazoles; D047428:Protein Kinase Inhibitors