5EM7
EGFR kinase domain mutant "TMLR" with pyridone compound 13: 4-[(2-methoxyphenyl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide
Summary for 5EM7
Entry DOI | 10.2210/pdb5em7/pdb |
Related | 5EM5 5EM6 5EM8 |
Descriptor | Epidermal growth factor receptor, SULFATE ION, 4-[(2-methoxyphenyl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide (3 entities in total) |
Functional Keywords | protein kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533 |
Total number of polymer chains | 1 |
Total formula weight | 38078.96 |
Authors | Eigenbrot, C.,Yu, C. (deposition date: 2015-11-05, release date: 2015-12-30, Last modification date: 2024-03-06) |
Primary citation | Bryan, M.C.,Burdick, D.J.,Chan, B.K.,Chen, Y.,Clausen, S.,Dotson, J.,Eigenbrot, C.,Elliott, R.,Hanan, E.J.,Heald, R.,Jackson, P.,La, H.,Lainchbury, M.,Malek, S.,Mann, S.E.,Purkey, H.E.,Schaefer, G.,Schmidt, S.,Seward, E.,Sideris, S.,Wang, S.,Yen, I.,Yu, C.,Heffron, T.P. Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR. Acs Med.Chem.Lett., 7:100-104, 2016 Cited by PubMed: 26819674DOI: 10.1021/acsmedchemlett.5b00428 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.81 Å) |
Structure validation
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