8UDV
The X-RAY co-crystal structure of human FGFR3 V555M and Compound 17
Summary for 8UDV
| Entry DOI | 10.2210/pdb8udv/pdb |
| Related | 8UDT 8UDU |
| Descriptor | Fibroblast growth factor receptor 3, SULFATE ION, 3-[(6-chloro-1-cyclopropyl-1H-benzimidazol-5-yl)ethynyl]-1-[(3S,5S)-5-(methoxymethyl)-1-(prop-2-enoyl)pyrrolidin-3-yl]-5-(methylamino)-1H-pyrazole-4-carboxamide, ... (5 entities in total) |
| Functional Keywords | fgfr inhibitor, covalent drug, kin-3248, alteration, mutation, structure-based drug design, kinase inhibitor, signaling, proliferation, transferase, transferase-inhibitor complex, transferase/inhibitor |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 3 |
| Total formula weight | 103628.79 |
| Authors | Tyhonas, J.S.,Arnold, L.D.,Cox, J.,Franovic, A.,Gardiner, E.,Grandinetti, K.,Kania, R.,Kanouni, T.,Lardy, M.,Li, C.,Martin, E.S.,Miller, N.,Mohan, A.,Murphy, E.A.,Perez, M.,Soroceanu, L.,Timple, N.,Uryu, S.,Womble, S.,Kaldor, S.W. (deposition date: 2023-09-29, release date: 2024-02-07, Last modification date: 2024-02-21) |
| Primary citation | Tyhonas, J.S.,Arnold, L.D.,Cox, J.M.,Franovic, A.,Gardiner, E.,Grandinetti, K.,Kania, R.,Kanouni, T.,Lardy, M.,Li, C.,Martin, E.S.,Miller, N.,Mohan, A.,Murphy, E.A.,Perez, M.,Soroceanu, L.,Timple, N.,Uryu, S.,Womble, S.,Kaldor, S.W. Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. J.Med.Chem., 67:1734-1746, 2024 Cited by PubMed: 38267212DOI: 10.1021/acs.jmedchem.3c01819 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.348 Å) |
Structure validation
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