Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

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Burns CJ, Bourke DG, Andrau L, Bu X, Charman SA, Donohue AC, Fantino E, Farrugia M, Feutrill JT, Joffe M, Kling MR, Kurek M, Nero TL, Nguyen T, Palmer JT, Phillips I, Shackleford DM, Sikanyika H, Styles M, Su S, Treutlein H, Zeng J, Wilks AF

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. doi: 10.1016/j.bmcl.2009.08.071. Epub 2009 Aug 23.

PubMed ID

19762238 [ View in PubMed

]

Abstract

A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tofacitinib	Tyrosine-protein kinase JAK2	IC 50 (nM)	33	N/A	N/A	Details
Tofacitinib	Tyrosine-protein kinase JAK3	IC 50 (nM)	5	N/A	N/A	Details