Discovery of highly potent, selective, covalent inhibitors of JAK3. Issue 20 (15th October 2017)

• Record Type: Journal Article
• Authors: Kempson, James; Ovalle, Damaso; Guo, Junqing; Wrobleski, Stephen T.; Lin, Shuqun; Spergel, Steven H.; Duan, James J.-W.; Jiang, Bin; Lu, Zhonghui; Das, Jagabandhu; Yang, Bingwei V.; Hynes, John; Wu, Hong; Tokarski, John; Sack, John S.; Khan, Javed; Schieven, Gary; Blatt, Yuval; Chaudhry, Charu; Salter-Cid, Luisa M.; Fura, Aberra; Barrish, Joel C.; Carter, Percy H.; Pitts, William J.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 20(2017)
• Page Start: 4622
• Page End: 4625
• Publication Date: 2017-10-15
• Subjects: JAK3 -- Covalent -- Irreversible inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.09.023
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.