3LZB

EGFR kinase domain complexed with an imidazo[2,1-b]thiazole inhibitor

Summary for 3LZB

• Entry DOI: 10.2210/pdb3lzb/pdb
• Descriptor: Epidermal growth factor receptor, N-[3-(5-{2-[(4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl}imidazo[2,1-b][1,3]thiazol-6-yl)phenyl]-2-phenylacetamide (3 entities in total)
• Functional Keywords: epidermal growth factor kinase domain, multitargeted small molecule 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: 8
• Total formula weight: 291450.65

Authors

Swinger, K.K. (deposition date: 2010-03-01, release date: 2011-03-02, Last modification date: 2023-09-06)

• Primary citation: Fidanze, S.D.,Erickson, S.A.,Wang, G.T.,Mantei, R.,Clark, R.F.,Sorensen, B.K.,Bamaung, N.Y.,Kovar, P.,Johnson, E.F.,Swinger, K.K.,Stewart, K.D.,Zhang, Q.,Tucker, L.A.,Pappano, W.N.,Wilsbacher, J.L.,Wang, J.,Sheppard, G.S.,Bell, R.L.,Davidsen, S.K.,Hubbard, R.D.; Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.; Bioorg.Med.Chem.Lett., 20:2452-2455, 2010; PubMed: 20346655; DOI: 10.1016/j.bmcl.2010.03.015

Experimental method

X-RAY DIFFRACTION (2.7 Å)