Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3)

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 5, 2007, Pages 1250-1253

  Clark, Michael P ^a,b   George, Kelly M ^a,b   Bookland, Roger G ^a,b   Chen, Jack ^a,b   Laughlin, Steven K ^a,b   Thakur, Kumar D ^a,b   Lee, Wenlin ^a,b   Davis, Jan R ^a,b   Cabrera, Ed J ^a,b   Brugel, Todd A ^a,b   VanRens, John C ^a,b   Laufersweiler, Matthew J ^a,b   Maier, Jennifer A ^a,b   Sabat, Mark P ^a,b   Golebiowski, Adam ^a,b   Easwaran, Vijay ^a,b   Webster, Mark E ^a,b   De, Biswanath ^a,b   Zhang, George ^a,b  

^a PROCTER AND GAMBLE PHARMACEUTICALS   (United States)

^b Metastatix Inc   (United States)

Author keywords

Cytokines; JAK3; Janus Kinase; Pyrrolopyrimidine; Tyrosine kinases

Indexed keywords

4 [N [1 (2 CYANO 1 OXOETHYL) 4 METHYL 3 PIPERIDINYL] N METHYLAMINO]PYRROLO[2,3 D]PYRIMIDINE; JANUS KINASE 3 INHIBITOR; PYRROLOPYRIMIDINE DERIVATIVE;

ARTICLE; ENZYME ACTIVITY; ENZYME INHIBITION;

AUTOIMMUNE DISEASES; CELL LINE, TUMOR; CELL PROLIFERATION; HUMANS; IMMUNITY; JANUS KINASE 2; JANUS KINASE 3; PYRIMIDINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33846900700     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.12.018     Document Type: Article

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8. ® Reagent) directly to a completed kinase reaction. This addition results in the generation of a luminescent signal correlated with the amount of ATP present and inversely proportional to the amount of kinase activity.
9. 50 = 6 nM).
10. 50s (Prism4 software).