3DBS
Structure of PI3K gamma in complex with GDC0941
Summary for 3DBS
Entry DOI | 10.2210/pdb3dbs/pdb |
Descriptor | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, 2-(1H-indazol-4-yl)-6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (2 entities in total) |
Functional Keywords | pi3k gamma, inhibitor, kinase, transferase |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 1 |
Total formula weight | 110411.84 |
Authors | Wiesmann, C.,Ultsch, M. (deposition date: 2008-06-02, release date: 2008-06-17, Last modification date: 2023-11-01) |
Primary citation | Folkes, A.J.,Ahmadi, K.,Alderton, W.K.,Alix, S.,Baker, S.J.,Box, G.,Chuckowree, I.S.,Clarke, P.A.,Depledge, P.,Eccles, S.A.,Friedman, L.S.,Hayes, A.,Hancox, T.C.,Kugendradas, A.,Lensun, L.,Moore, P.,Olivero, A.G.,Pang, J.,Patel, S.,Pergl-Wilson, G.H.,Raynaud, F.I.,Robson, A.,Saghir, N.,Salphati, L.,Sohal, S.,Ultsch, M.H.,Valenti, M.,Wallweber, H.J.A.,Wan, N.C.,Wiesmann, C.,Workman, P.,Zhyvoloup, A.,Zvelebil, M.J.,Shuttleworth, S.J. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer J.Med.Chem., 51:5522-5532, 2008 Cited by PubMed: 18754654DOI: 10.1021/jm800295d PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.8 Å) |
Structure validation
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