Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase
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
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)
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase
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.
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)
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase
Optimization of the ADME properties of a series of 2,4-diaminopyrimidine-5- carboxamide inhibitors of Sky kinase resulted in the identification of highly selective compounds with properties suitable for use as in vitro and in vivo tools to probe the effects of Sky inhibition.
Powell, Noel A.,Hoffman, Jennifer K.,Ciske, Fred L.,Kohrt, Jeffrey T.,Baxi, Sangita M.,Peng, Yun-Wen,Zhong, Min,Catana, Cornel,Ohren, Jeff,Perrin, Lisa A.,Edmunds, Jeremy J.
p. 1051 - 1055
(2013/03/13)
More Articles about upstream products of 1421367-66-9