4R1V

Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors

Summary for 4R1V

• Entry DOI: 10.2210/pdb4r1v/pdb
• Related: 4R1Y
• Descriptor: Hepatocyte growth factor receptor, 3-[1-(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}benzyl)-6-oxo-1,6-dihydropyridazin-3-yl]benzonitrile, GAMMA-BUTYROLACTONE, ... (4 entities in total)
• Functional Keywords: protein kinase, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Membrane; Single-pass type I membrane protein. Isoform 3: Secreted: P08581
• Total number of polymer chains: 1
• Total formula weight: 33742.21

Authors

Blaukat, A.,Bladt, F.,Friese-Hamim, M.,Knuehl, C.,Fittschen, C.,Graedler, U.,Meyring, M.,Dorsch, D.,Stieber, F.,Schadt, O. (deposition date: 2014-08-07, release date: 2015-03-18, Last modification date: 2024-02-28)

• Primary citation: Dorsch, D.,Schadt, O.,Stieber, F.,Meyring, M.,Gradler, U.,Bladt, F.,Friese-Hamim, M.,Knuhl, C.,Pehl, U.,Blaukat, A.; Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.; Bioorg.Med.Chem.Lett., 25:1597-1602, 2015; PubMed: 25736998; DOI: 10.1016/j.bmcl.2015.02.002

Experimental method

X-RAY DIFFRACTION (1.2 Å)