7KHK
Crystal structure of KIT kinase domain with a small molecule inhibitor, PLX9486 (bezuclastinib) in the DFG-in state
Summary for 7KHK
Entry DOI | 10.2210/pdb7khk/pdb |
Related | 7KHG 7KHJ |
Descriptor | Mast/stem cell growth factor receptor Kit, 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide (3 entities in total) |
Functional Keywords | transferase, tyrosine-protein kinase, atp-binding, kinase-kinase inhibitor complex, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 2 |
Total formula weight | 76630.87 |
Authors | Zhang, Y. (deposition date: 2020-10-21, release date: 2021-07-07, Last modification date: 2023-10-18) |
Primary citation | Wagner, A.J.,Severson, P.L.,Shields, A.F.,Patnaik, A.,Chugh, R.,Tinoco, G.,Wu, G.,Nespi, M.,Lin, J.,Zhang, Y.,Ewing, T.,Habets, G.,Burton, E.A.,Matusow, B.,Tsai, J.,Tsang, G.,Shellooe, R.,Carias, H.,Chan, K.,Rezaei, H.,Sanftner, L.,Marimuthu, A.,Spevak, W.,Ibrahim, P.N.,Inokuchi, K.,Alcantar, O.,Michelson, G.,Tsiatis, A.C.,Zhang, C.,Bollag, G.,Trent, J.C.,Tap, W.D. Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial. Jama Oncol, 7:1343-1350, 2021 Cited by PubMed: 34236401DOI: 10.1001/jamaoncol.2021.2086 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.34 Å) |
Structure validation
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