1421367-68-1Relevant articles and documents
Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase
Aydogan, Yagmur,Berger, Benedict-Tilman,Chaikuad, Apirat,Drewry, David H.,Knapp, Stefan,Müller, Susanne,Mandel, Sebastian,Mauer, Sandy,Pohl, Christian,Russ, Nadine,Schr?der, Martin
, p. 14358 - 14376 (2021/10/12)
CASK (Ca2+/calmodulin-dependent Ser/Thr kinase) is a member of the MAGUK (membrane-associated guanylate kinase) family that functions as neurexin kinases with roles implicated in neuronal synapses and trafficking. The lack of a canonical DFG motif, which
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase
Powell, Noel A.,Hoffman, Jennifer K.,Ciske, Fred L.,Kaufman, Michael D.,Kohrt, Jeffrey T.,Quin III, John,Sheehan, Derek J.,Delaney, Amy,Baxi, Sangita M.,Catana, Cornel,McConnell, Patrick,Ohren, Jeff,Perrin, Lisa A.,Edmunds, Jeremy J.
, p. 1046 - 1050 (2013/03/14)
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.