3IO7

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2

Summary for 3IO7

• Entry DOI: 10.2210/pdb3io7/pdb
• Descriptor: Tyrosine-protein kinase JAK2, (3S)-1-[6-(2-aminopyrazolo[1,5-a]pyrimidin-3-yl)pyrimidin-4-yl]-N,N-diethylpiperidine-3-carboxamide (3 entities in total)
• Functional Keywords: kinase, inhibitor, jak2, janus kinase, atp-binding, chromosomal rearrangement, disease mutation, membrane, nucleotide-binding, phosphoprotein, polymorphism, proto-oncogene, sh2 domain, transferase, tyrosine-protein kinase
• Biological source: Homo sapiens (human)
• Cellular location: Endomembrane system ; Peripheral membrane protein : O60674
• Total number of polymer chains: 1
• Total formula weight: 37177.28

Authors

Zuccola, H.J.,Ledeboer, M.W.,Pierce, A.C. (deposition date: 2009-08-13, release date: 2009-11-10, Last modification date: 2024-03-13)

• Primary citation: Ledeboer, M.W.,Pierce, A.C.,Duffy, J.P.,Gao, H.,Messersmith, D.,Salituro, F.G.,Nanthakumar, S.,Come, J.,Zuccola, H.J.,Swenson, L.,Shlyakter, D.,Mahajan, S.,Hoock, T.,Fan, B.,Tsai, W.J.,Kolaczkowski, E.,Carrier, S.,Hogan, J.K.,Zessis, R.,Pazhanisamy, S.,Bennani, Y.L.; 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.; Bioorg.Med.Chem.Lett., 19:6529-6533, 2009; PubMed: 19857967; DOI: 10.1016/j.bmcl.2009.10.053

Experimental method

X-RAY DIFFRACTION (2.6 Å)