3QKM
Spirocyclic sulfonamides as AKT inhibitors
Summary for 3QKM
Entry DOI | 10.2210/pdb3qkm/pdb |
Related | 3OCB |
Descriptor | RAC-alpha serine/threonine-protein kinase, N-(2-ethoxyethyl)-N-{(2S)-2-hydroxy-3-[(5R)-2-(quinazolin-4-yl)-2,7-diazaspiro[4.5]dec-7-yl]propyl}-2,6-dimethylbenzenesulfonamide (3 entities in total) |
Functional Keywords | kinase domain, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Cytoplasm: P31749 |
Total number of polymer chains | 1 |
Total formula weight | 40048.74 |
Authors | Xu, R.,Banka, A.,Blake, J.F.,Mitchell, I.S.,Wallace, E.M.,Gloor, S.L.,Martinson, M.,Risom, T.,Gross, S.D.,Morales, T.,Vigers, G.P.A.,Brandhuber, B.J.,Skelton, N.J. (deposition date: 2011-02-01, release date: 2011-04-06, Last modification date: 2011-07-13) |
Primary citation | Xu, R.,Banka, A.,Blake, J.F.,Mitchell, I.S.,Wallace, E.M.,Bencsik, J.R.,Kallan, N.C.,Spencer, K.L.,Gloor, S.L.,Martinson, M.,Risom, T.,Gross, S.D.,Morales, T.H.,Wu, W.I.,Vigers, G.P.,Brandhuber, B.J.,Skelton, N.J. Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA. Bioorg.Med.Chem.Lett., 21:2335-2340, 2011 Cited by PubMed: 21420856DOI: 10.1016/j.bmcl.2011.02.098 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.2 Å) |
Structure validation
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