Fragment-based discovery of JAK-2 inhibitors.
Article Details
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Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M
Fragment-based discovery of JAK-2 inhibitors.
Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22.
- PubMed ID
- 19019674 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 4-(3-amino-1H-indazol-5-yl)-N-tert-butylbenzenesulfonamide Tyrosine-protein kinase JAK2 IC 50 (nM) 78 N/A N/A Details 5-phenyl-1H-indazol-3-amine Tyrosine-protein kinase JAK2 IC 50 (nM) 1600 N/A N/A Details