Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design
Interleukin-2 inducible T-cell kinase (ITK) is a member of the Tec kinase family and is involved with T-cell activation and proliferation. Due to its critical role in acting as a modulator of T-cells, ITK inhibitors could provide a novel route to anti-inf
Cook, Brian N.,Bentzien, J?rg,White, Andre,Nemoto, Peter A.,Wang, Ji,Man, Chuk C.,Soleymanzadeh, Fariba,Khine, Hnin Hnin,Kashem, Mohammed A.,Kugler Jr., Stanley Z.,Wolak, John P.,Roth, Gregory P.,De Lombaert, Stéphane,Pullen, Steven S.,Takahashi, Hidenori
scheme or table
p. 773 - 777
(2009/08/15)
Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead
Previously, we reported a series of novel benzimidazole based Itk inhibitors that exhibited excellent enzymatic potency and selectivity but low microsomal stability. Employing a structure based approach a new series of inhibitors with comparable potency a
Moriarty, Kevin J.,Winters, Michael,Qiao, Lei,Ryan, Declan,DesJarlis, Renee,Robinson, Darius,Cook, Brian N.,Kashem, Mohammed A.,Kaplita, Paul V.,Liu, Lisa H.,Farrell, Thomas M.,Khine, Hnin Hnin,King, Josephine,Pullen, Steven S.,Roth, Gregory P.,Magolda, Ronald,Takahashi, Hidenori
scheme or table
p. 5537 - 5540
(2009/06/30)
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