3IOK

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

Summary for 3IOK

• Entry DOI: 10.2210/pdb3iok/pdb
• Related: 3IO7
• Descriptor: Tyrosine-protein kinase JAK2, 3-(6-{[(1S)-1-(4-fluorophenyl)ethyl]amino}pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine (3 entities in total)
• Functional Keywords: kinase, inhibitor, jak2, janus kinase, atp-binding, disease mutation, membrane, nucleotide-binding, phosphoprotein, proto-oncogene, sh2 domain, transferase, tyrosine-protein kinase
• Biological source: Homo sapiens (human)
• Cellular location: Endomembrane system; Peripheral membrane protein (By similarity): O60674
• Total number of polymer chains: 1
• Total formula weight: 37132.17

Authors

Zuccola, H.J.,Ledeboer, M.W.,Pierce, A.C. (deposition date: 2009-08-14, release date: 2009-11-10, Last modification date: 2013-04-03)

• 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 (2.1 Å)