1110502-41-4Relevant articles and documents
Fragment-based discovery of JAK-2 inhibitors
Antonysamy, Stephen,Hirst, Gavin,Park, Frances,Sprengeler, Paul,Stappenbeck, Frank,Steensma, Ruo,Wilson, Mark,Wong, Melissa
scheme or table, p. 279 - 282 (2009/04/16)
Fragment-based hit identification coupled with crystallographically enabled structure-based drug design was used to design potent inhibitors of JAK-2. After two iterations from fragment 1, we were able to increase potency by greater than 500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
