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Discovery of highly potent, selective, covalent inhibitors of JAK3.

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, Charu Chaudhry, Luisa M Salter-Cid, Aberra Fura, Joel C Barrish, Percy H Carter, William J Pitts
Bioorganic & Medicinal Chemistry Letters 2017 October 16
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.

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