Download MendeleyDiscovery of highly potent, selective, covalent inhibitors of JAK3.
Kempson, J., Ovalle, D., Guo, J., Wrobleski, S.T., Lin, S., Spergel, S.H., Duan, J.J., Jiang, B., Lu, Z., Das, J., Yang, B.V., Hynes, J., Wu, H., Tokarski, J., Sack, J.S., Khan, J., Schieven, G., Blatt, Y., Chaudhry, C., Salter-Cid, L.M., Fura, A., Barrish, J.C., Carter, P.H., Pitts, W.J.(2017) Bioorg Med Chem Lett 27: 4622-4625
- PubMed: 28927786
- DOI: https://doi.org/10.1016/j.bmcl.2017.09.023
- Primary Citation of Related Structures:
5WFJ - PubMed 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.
Organizational Affiliation:
Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA. Electronic address: james.kempson@bms.com.
