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4EZL

Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf

Summary for 4EZL
Entry DOI10.2210/pdb4ezl/pdb
Related4EZJ 4EZK
DescriptorPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, 2-(1-{[2-(2-aminopyrimidin-5-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl}piperidin-4-yl)propan-2-ol (3 entities in total)
Functional Keywordskinase p110, p110-gamma, lipid kinase, cytoplasmic, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (human)
Cellular locationCytoplasm: P48736
Total number of polymer chains1
Total formula weight111163.59
Authors
Murray, J.M. (deposition date: 2012-05-02, release date: 2013-04-17, Last modification date: 2023-09-13)
Primary citationSutherlin, 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: 22672799
DOI: 10.1016/j.bmcl.2012.05.027
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.94 Å)
Structure validation

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