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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）

Cited 24|Views68
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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.
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Key words
JAK3,Covalent,Irreversible inhibitor
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