title: 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.
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.
authors.affiliation: Genentech, Inc, 1 DNA Way, South San Francisco, CA 94080, United States. siu.michael@gene.com
authors.forename: Michael
authors.initials: M
authors.lastname: Siu
authors.forename: Richard
authors.initials: R
authors.lastname: Pastor
authors.forename: Wendy
authors.initials: W
authors.lastname: Liu
authors.forename: Kathy
authors.initials: K
authors.lastname: Barrett
authors.forename: Megan
authors.initials: M
authors.lastname: Berry
authors.forename: Wade S
authors.initials: WS
authors.lastname: Blair
authors.forename: Christine
authors.initials: C
authors.lastname: Chang
authors.forename: Jacob Z
authors.initials: JZ
authors.lastname: Chen
authors.forename: Charles
authors.initials: C
authors.lastname: Eigenbrot
authors.forename: Nico
authors.initials: N
authors.lastname: Ghilardi
authors.forename: Paul
authors.initials: P
authors.lastname: Gibbons
authors.forename: Haiying
authors.initials: H
authors.lastname: He
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Hurley
authors.forename: Jane R
authors.initials: JR
authors.lastname: Kenny
authors.forename: S
authors.initials: S
authors.lastname: Cyrus Khojasteh
authors.forename: Hoa
authors.initials: H
authors.lastname: Le
authors.forename: Leslie
authors.initials: L
authors.lastname: Lee
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Lyssikatos
authors.forename: Steve
authors.initials: S
authors.lastname: Magnuson
authors.forename: Rebecca
authors.initials: R
authors.lastname: Pulk
authors.forename: Vickie
authors.initials: V
authors.lastname: Tsui
authors.forename: Mark
authors.initials: M
authors.lastname: Ultsch
authors.forename: Yisong
authors.initials: Y
authors.lastname: Xiao
authors.forename: Bing-yan
authors.initials: BY
authors.lastname: Zhu
authors.forename: Deepak
authors.initials: D
authors.lastname: Sampath
mesh_terms: D000640:Amitrole / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D018360:Crystallography, X-Ray; D006801:Humans; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D051379:Mice; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: C494034:1,2,4-triazolo(1,5-c)pyrimidine; D000970:Antineoplastic Agents; D011743:Pyrimidines; D014230:Triazoles; D053614:Janus Kinase 2; D000640:Amitrole
keywords: JAK2; Janus kinase; Triazolopyridine