Insights into the modular design of kinase inhibitors and application to Abl and Axl

Scaffold hopping is a common strategy for generating kinase inhibitors that bind to the DFG-out inactive conformation. Small structural differences in inhibitor scaffolds can have significant effects on potency and selectivity across the kinome, however, these effects are often not studied in detail...

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Veröffentlicht in:	MedChemComm 2022-01, Vol.13 (1), p.64-71
Hauptverfasser:	Phadke, Sameer, Lopez-Barcons, Lluis, Vandecan, Nathalie, Wu, Zhifen, Johnson, Taylor K, Lachacz, Eric J, Merajver, Sofia D, Soellner, Matthew B
Format:	Artikel
Sprache:	eng
Schlagworte:	Axl protein Binders Chemistry Conformation Inhibitors Kinases Modular design Scaffolds Selectivity
Online-Zugang:	Volltext
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