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Discovery of highly potent,selective, covalent inhibitors of JAK3
Authors:James Kempson  Damaso Ovalle  Junqing Guo  Stephen T. Wrobleski  Shuqun Lin  Steven H. Spergel  James J.-W. Duan  Bin Jiang  Zhonghui Lu  Jagabandhu Das  Bingwei V. Yang  John Hynes  Hong Wu  John Tokarski  John S. Sack  Javed Khan  Gary Schieven  Yuval Blatt  William J. Pitts
Affiliation:Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA
Abstract:A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design was based on crystal structure information and a comparative study of several electrophilic warheads.
Keywords:JAK3  Covalent  Irreversible inhibitor
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