5ECE
Tankyrase 1 with Phthalazinone 1
Summary for 5ECE
Entry DOI | 10.2210/pdb5ece/pdb |
Descriptor | Tankyrase-1, 1,2-ETHANEDIOL, 2-[4-[3-[(4-oxidanylidene-3~{H}-phthalazin-1-yl)methyl]phenyl]carbonylpiperazin-1-yl]pyridine-3-carbonitrile, ... (6 entities in total) |
Functional Keywords | tankyrase, inhibitor, parp, centrosome clustering, oncology, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm: O95271 |
Total number of polymer chains | 4 |
Total formula weight | 99328.87 |
Authors | Kazmirski, S.L.,Johannes, J.,Read, J.A.,Howard, T.,Larsen, N.A.,Ferguson, A.D. (deposition date: 2015-10-20, release date: 2015-11-25, Last modification date: 2024-03-06) |
Primary citation | Johannes, J.W.,Almeida, L.,Daly, K.,Ferguson, A.D.,Grosskurth, S.E.,Guan, H.,Howard, T.,Ioannidis, S.,Kazmirski, S.,Lamb, M.L.,Larsen, N.A.,Lyne, P.D.,Mikule, K.,Ogoe, C.,Peng, B.,Petteruti, P.,Read, J.A.,Su, N.,Sylvester, M.,Throner, S.,Wang, W.,Wang, X.,Wu, J.,Ye, Q.,Yu, Y.,Zheng, X.,Scott, D.A. Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering. Bioorg.Med.Chem.Lett., 25:5743-5747, 2015 Cited by PubMed: 26546219DOI: 10.1016/j.bmcl.2015.10.079 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.2 Å) |
Structure validation
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