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Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

[Image: see text] Fragment screening of phosphoinositide-dependent kinase-1 (PDK1) in a biochemical kinase assay afforded hits that were characterized and prioritized based on ligand efficiency and binding interactions with PDK1 as determined by NMR. Subsequent crystallography and follow-up screenin...

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Detalhes bibliográficos
Main Authors: Medina, Jesús R., Blackledge, Charles W., Heerding, Dirk A., Campobasso, Nino, Ward, Paris, Briand, Jacques, Wright, Lois, Axten, Jeffrey M.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2010
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4007849/
https://ncbi.nlm.nih.gov/pubmed/24900229
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml100136n
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