Fragment-based discovery of JAK-2 inhibitors.

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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

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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