Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic …

…, E Kieras, W Stochaj, L Mosyak, J McKew…

文献索引：Moy, Franklin J.; Lee, Arthur; Gavrin, Lori Krim; Xu, Zhang Bao; Sievers, Annette; Kieras, Elizabeth; Stochaj, Wayne; Mosyak, Lidia; McKew, John; Tsao, Desiree H. H. Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1238 - 1249

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被引用次数: 19

摘要

To aid in the pursuit of selective kinase inhibitors, we have developed a unique ATP site binder tool for the detection of binders outside the ATP site by nuclear magnetic resonance (NMR). We report here the novel synthesis that led to this paramagnetic spin-labeled pyrazolopyrimidine probe (1), which exhibits nanomolar inhibitory activity against multiple kinases. We demonstrate the application of this probe by performing NMR binding ...