6D8E

Discovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor

Summary for 6D8E

• Entry DOI: 10.2210/pdb6d8e/pdb
• Descriptor: Epidermal growth factor receptor, (4-fluorophenyl)methyl {2-[(1-methyl-1H-pyrazol-3-yl)amino]pyrimidin-4-yl}[3-(propanoylamino)phenyl]carbamate (3 entities in total)
• Functional Keywords: egfr, inhibitor, signaling protein, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 37793.63

Authors

Park, E.,Eck, M.J. (deposition date: 2018-04-26, release date: 2018-07-18, Last modification date: 2023-10-04)

• Primary citation: Jang, J.,Son, J.,Park, E.,Kosaka, T.,Saxon, J.A.,De Clercq, D.J.H.,Choi, H.G.,Tanizaki, J.,Eck, M.J.,Janne, P.A.,Gray, N.S.; Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.; Angew. Chem. Int. Ed. Engl., 57:11629-11633, 2018; PubMed: 29978938; DOI: 10.1002/anie.201805187

Experimental method

X-RAY DIFFRACTION (2.537 Å)