3KCK
A Novel Chemotype of Kinase Inhibitors
Summary for 3KCK
Entry DOI | 10.2210/pdb3kck/pdb |
Descriptor | Tyrosine-protein kinase JAK2, 3-chloro-4-(4H-3,4,7-triazadibenzo[cd,f]azulen-6-yl)phenol (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 (By similarity): O60674 |
Total number of polymer chains | 1 |
Total formula weight | 37128.59 |
Authors | Zuccola, H.J.,Wang, T.,Ledeboer, M.W. (deposition date: 2009-10-21, release date: 2009-11-24, Last modification date: 2011-07-13) |
Primary citation | Wang, T.,Ledeboer, M.W.,Duffy, J.P.,Pierce, A.C.,Zuccola, H.J.,Block, E.,Shlyakter, D.,Hogan, J.K.,Bennani, Y.L. A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors. Bioorg.Med.Chem.Lett., 20:153-156, 2010 Cited by PubMed: 19945871DOI: 10.1016/j.bmcl.2009.11.021 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.2 Å) |
Structure validation
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