5K0X
Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC2541
Summary for 5K0X
Entry DOI | 10.2210/pdb5k0x/pdb |
Related | 5K0K |
Descriptor | Tyrosine-protein kinase Mer, CHLORIDE ION, (7S)-7-amino-N-[(4-fluorophenyl)methyl]-8-oxo-2,9,16,18,21-pentaazabicyclo[15.3.1]henicosa-1(21),17,19-triene-20-carboxamide, ... (4 entities in total) |
Functional Keywords | macrocyclic, drug design, fibrinolytic agents, protein kinase inhibitors, proto-oncogene proteins, pyrimidines, receptor protein-tyrosine kinases, structure-activity relationship, thrombosis, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Membrane ; Single-pass type I membrane protein : Q12866 |
Total number of polymer chains | 2 |
Total formula weight | 72899.28 |
Authors | McIver, A.L.,Zhang, W.,Liu, Q.,Jiang, X.,Stashko, M.A.,Nichols, J.,Miley, M.J.,Norris-Drouin, J.,Machius, M.,DeRyckere, D.,Wood, E.,Graham, D.K.,Earp, H.S.,Kireev, D.,Frye, S.V.,Wang, X. (deposition date: 2016-05-17, release date: 2017-02-22, Last modification date: 2023-09-27) |
Primary citation | McIver, A.L.,Zhang, W.,Liu, Q.,Jiang, X.,Stashko, M.A.,Nichols, J.,Miley, M.J.,Norris-Drouin, J.,Machius, M.,DeRyckere, D.,Wood, E.,Graham, D.K.,Earp, H.S.,Kireev, D.,Frye, S.V.,Wang, X. Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors. ChemMedChem, 12:207-213, 2017 Cited by PubMed: 28032464DOI: 10.1002/cmdc.201600589 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.231 Å) |
Structure validation
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