5HCZ

EGFR kinase domain mutant "TMLR" with 3-azetidinyl azaindazole compound 21

5HCZ の概要

• エントリーDOI: 10.2210/pdb5hcz/pdb
• 関連するPDBエントリー: 5HCX 5HCY
• 分子名称: Epidermal growth factor receptor, SULFATE ION, 2-[1-[1-[(2~{S})-butan-2-yl]-6-[[2-(1-cyclopropylsulfonylpyrazol-4-yl)pyrimidin-4-yl]amino]pyrazolo[4,3-c]pyridin-3-yl]azetidin-3-yl]propan-2-ol, ... (4 entities in total)
• 機能のキーワード: protein kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 38197.13

構造登録者

Eigenbrot, C.,Yu, C. (登録日: 2016-01-04, 公開日: 2016-09-07, 最終更新日: 2023-09-27)

• 主引用文献: Chan, B.K.,Hanan, E.J.,Bowman, K.K.,Bryan, M.C.,Burdick, D.,Chan, E.,Chen, Y.,Clausen, S.,Dela Vega, T.,Dotson, J.,Eigenbrot, C.,Elliott, R.L.,Heald, R.A.,Jackson, P.S.,Knight, J.D.,La, H.,Lainchbury, M.D.,Malek, S.,Purkey, H.E.,Schaefer, G.,Schmidt, S.,Seward, E.M.,Sideris, S.,Shao, L.,Wang, S.,Yeap, S.K.,Yen, I.,Yu, C.,Heffron, T.P.; Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.; J.Med.Chem., 59:9080-9093, 2016; PubMed: 27564586; DOI: 10.1021/acs.jmedchem.6b00995

実験手法

X-RAY DIFFRACTION (2.62 Å)