Fragment-based discovery of JAK-2 inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
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.
- Research Organization:
- Argonne National Laboratory (ANL)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1005713
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (1) ; 01, 2009 Vol. 19; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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