4R5Y
The complex structure of Braf V600E kinase domain with a novel Braf inhibitor
Summary for 4R5Y
Entry DOI | 10.2210/pdb4r5y/pdb |
Descriptor | Serine/threonine-protein kinase B-raf, 5-({(1R,1aS,6bR)-1-[5-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl}oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one (2 entities in total) |
Functional Keywords | kinase, signal transduction, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Nucleus : P15056 |
Total number of polymer chains | 2 |
Total formula weight | 67607.11 |
Authors | |
Primary citation | Tang, Z.,Yuan, X.,Du, R.,Cheung, S.H.,Zhang, G.,Wei, J.,Zhao, Y.,Feng, Y.,Peng, H.,Zhang, Y.,Du, Y.,Hu, X.,Gong, W.,Liu, Y.,Gao, Y.,Liu, Y.,Hao, R.,Li, S.,Wang, S.,Ji, J.,Zhang, L.,Li, S.,Sutton, D.,Wei, M.,Zhou, C.,Wang, L.,Luo, L. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol.Cancer Ther., 14:2187-2197, 2015 Cited by PubMed: 26208524DOI: 10.1158/1535-7163.MCT-15-0262 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (3.5 Å) |
Structure validation
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