5K0K
Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC2434
Summary for 5K0K
Entry DOI | 10.2210/pdb5k0k/pdb |
Related | 5K0X |
Descriptor | Tyrosine-protein kinase Mer, CHLORIDE ION, 15-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}-4,5,6,7,9,10,11,12-octahydro-2,16-(azenometheno)pyrrolo[2,1-d][1,3,5,9]te traazacyclotetradecin-8(3H)-one, ... (5 entities in total) |
Functional Keywords | macrocyclic, pyrrolopyrimidines, 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 | 72939.09 |
Authors | Wang, X.,Liu, J.,Zhang, W.,Stashko, M.A.,Nichols, J.,DeRyckere, D.,Miley, M.J.,Norris-Drouin, J.,Chen, Z.,Machius, M.,Wood, E.,Graham, D.K.,Earp, H.S.,Graham, K.,Kireev, D.,Frye, S.V. (deposition date: 2016-05-17, release date: 2017-01-11, Last modification date: 2023-09-27) |
Primary citation | Wang, X.,Liu, J.,Zhang, W.,Stashko, M.A.,Nichols, J.,Miley, M.J.,Norris-Drouin, J.,Chen, Z.,Machius, M.,DeRyckere, D.,Wood, E.,Graham, D.K.,Earp, H.S.,Kireev, D.,Frye, S.V. Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors. ACS Med Chem Lett, 7:1044-1049, 2016 Cited by PubMed: 27994735DOI: 10.1021/acsmedchemlett.6b00221 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.545 Å) |
Structure validation
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