5P9F
BTK IN COMPLEX WITH GDC-0834
Summary for 5P9F
Entry DOI | 10.2210/pdb5p9f/pdb |
Group deposition | Crystal structures of Tyrosine-protein kinase BTK in complex with inhibitors (G_1002011) |
Descriptor | Tyrosine-protein kinase BTK, N-{3-[6-({4-[(2R)-1,4-dimethyl-3-oxopiperazin-2-yl]phenyl}amino)-4-methyl-5-oxo-4,5-dihydropyrazin-2-yl]-2-methylphenyl }-4,5,6,7-tetrahydro-1-benzothiophene-2-carboxamide, 1,2-ETHANEDIOL, ... (5 entities in total) |
Functional Keywords | lead optimization, protein kinase, transferase |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm: Q06187 |
Total number of polymer chains | 1 |
Total formula weight | 33263.18 |
Authors | Gardberg, A.S. (deposition date: 2016-09-20, release date: 2017-05-24, Last modification date: 2024-05-22) |
Primary citation | Bender, A.T.,Gardberg, A.,Pereira, A.,Johnson, T.,Wu, Y.,Grenningloh, R.,Head, J.,Morandi, F.,Haselmayer, P.,Liu-Bujalski, L. Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling. Mol. Pharmacol., 91:208-219, 2017 Cited by PubMed: 28062735DOI: 10.1124/mol.116.107037 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.71 Å) |
Structure validation
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