4EZK
Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf
Summary for 4EZK
Entry DOI | 10.2210/pdb4ezk/pdb |
Related | 4EZJ 4EZL |
Descriptor | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, 2-(1-{[2-(2H-indazol-4-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl}piperidin-4-yl)propan-2-ol (3 entities in total) |
Functional Keywords | kinase p110, p110-gamma, lipid kinase, cytoplasmic, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Cytoplasm: P48736 |
Total number of polymer chains | 1 |
Total formula weight | 111186.62 |
Authors | Murray, J.M. (deposition date: 2012-05-02, release date: 2013-04-17, Last modification date: 2023-09-13) |
Primary citation | Sutherlin, D.P.,Baker, S.,Bisconte, A.,Blaney, P.M.,Brown, A.,Chan, B.K.,Chantry, D.,Castanedo, G.,DePledge, P.,Goldsmith, P.,Goldstein, D.M.,Hancox, T.,Kaur, J.,Knowles, D.,Kondru, R.,Lesnick, J.,Lucas, M.C.,Lewis, C.,Murray, J.,Nadin, A.J.,Nonomiya, J.,Pang, J.,Pegg, N.,Price, S.,Reif, K.,Safina, B.S.,Salphati, L.,Staben, S.,Seward, E.M.,Shuttleworth, S.,Sohal, S.,Sweeney, Z.K.,Ultsch, M.,Waszkowycz, B.,Wei, B. Potent and selective inhibitors of PI3K-delta: obtaining isoform selectivity from the affinity pocket and tryptophan shelf Bioorg.Med.Chem.Lett., 22:4296-4302, 2012 Cited by PubMed: 22672799DOI: 10.1016/j.bmcl.2012.05.027 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.803 Å) |
Structure validation
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