2. Academic Validation
  3. 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

  • Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008.
Michael Siu 1,  Richard Pastor,  Wendy Liu,  Kathy Barrett,  Megan Berry,  Wade S Blair,  Christine Chang,  Jacob Z Chen,  Charles Eigenbrot,  Nico Ghilardi,  Paul Gibbons,  Haiying He,  Christopher A Hurley,  Jane R Kenny,  S Cyrus Khojasteh,  Hoa Le,  Leslie Lee,  Joseph P Lyssikatos,  Steve Magnuson,  Rebecca Pulk,  Vickie Tsui,  Mark Ultsch,  Yisong Xiao,  Bing-yan Zhu,  Deepak Sampath
Affiliations

Affiliation

  • 1 Genentech, Inc, 1 DNA Way, South San Francisco, CA 94080, United States. siu.michael@gene.com
PMID: 23870430 DOI: 10.1016/j.bmcl.2013.06.008
Abstract

The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 Inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed.

Keywords

JAK2; Janus kinase; Triazolopyridine.

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