3L8V

Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor C-MET in complex with a biarylamine based inhibitor

3L8V の概要

分子名称Hepatocyte growth factor receptor, 2-({4-[(2-aminopyridin-4-yl)oxy]-3-fluorophenyl}amino)-N-(2,4-difluorophenyl)pyridine-3-carboxamide (3 entities in total)
機能のキーワードreceptor tyrosine kinase, signal transduction, grb2, shc, atp-binding, glycoprotein, membrane, nucleotide-binding, phosphoprotein, proto-oncogene, transferase, transmembrane, tyrosine-protein kinase, alternative splicing, chromosomal rearrangement, disease mutation, kinase, polymorphism, receptor
由来する生物種Homo sapiens (human)
細胞内の位置Membrane; Single-pass type I membrane protein. Isoform 3: Secreted P08581
ポリマー鎖数1
分子量合計35886.43
構造登録者
Sack, J. (登録日: 2010-01-04, 公開日: 2010-05-05, 最終更新日: 2018-03-14)
主引用文献
Williams, D.K.,Chen, X.T.,Tarby, C.,Kaltenbach, R.,Cai, Z.W.,Tokarski, J.S.,An, Y.,Sack, J.S.,Wautlet, B.,Gullo-Brown, J.,Henley, B.J.,Jeyaseelan, R.,Kellar, K.,Manne, V.,Trainor, G.L.,Lombardo, L.J.,Fargnoli, J.,Borzilleri, R.M.
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
Bioorg.Med.Chem.Lett., 20:2998-3002, 2010
PubMed: 20382527 (主引用文献が同じPDBエントリー)
DOI: 10.1016/j.bmcl.2010.01.042
MImport into Mendeley
実験手法
X-RAY DIFFRACTION (2.4 Å)
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構造検証レポート

ClashscoreRamachandran outliersSidechain outliersRSRZ outliers22.8%6.2%8.5%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution
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