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5EM5

EGFR kinase domain mutant "TMLR" with pyridone compound 2: 4-[2-(4-chlorophenyl)ethylamino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide

Summary for 5EM5
Entry DOI10.2210/pdb5em5/pdb
Related5EM6 5EM7 5EM8
DescriptorEpidermal growth factor receptor, 4-[2-(4-chlorophenyl)ethylamino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide (3 entities in total)
Functional Keywordsprotein kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationCell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533
Total number of polymer chains1
Total formula weight38015.37
Authors
Eigenbrot, C.,Yu, C. (deposition date: 2015-11-05, release date: 2015-12-30, Last modification date: 2024-03-06)
Primary citationBryan, 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: 26819674
DOI: 10.1021/acsmedchemlett.5b00428
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.65 Å)
Structure validation

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