3A4P

human c-MET kinase domain complexed with 6-benzyloxyquinoline inhibitor

Summary for 3A4P

• Entry DOI: 10.2210/pdb3a4p/pdb
• Related: 1r1w 2wgj
• Descriptor: Hepatocyte growth factor receptor, CHLORIDE ION, ISOPROPYL ALCOHOL, ... (5 entities in total)
• Functional Keywords: c-met, tyrosine-protein kinase, hepatocyte growth factor receptor, transferase
• 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: 36562.61

Authors

Fukami, T.A.,Kadono, S.,Yamamuro, M.,Matsuura, T. (deposition date: 2009-07-13, release date: 2010-02-16, Last modification date: 2023-11-01)

Primary citation

Nishii, H.,Chiba, T.,Morikami, K.,Fukami, T.A.,Sakamoto, H.,Ko, K.,Koyano, H.
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors
Bioorg.Med.Chem.Lett., 20:1405-1409, 2010

PubMed Abstract: A novel quinoline derivative that selectively inhibits c-Met kinase was identified. The molecular design is based on a result of the analysis of a PF-2341066 (1)/c-Met cocrystal structure (PDB code: 2wgj). The kinase selectivity of the derivatives is discussed from the view point of the sequence homology of the kinases, the key interactions found in X-ray cocrystal structures, and the structure-activity relationship (SAR) obtained in this work.

PubMed: 20093027
DOI: 10.1016/j.bmcl.2009.12.109

Experimental method

X-RAY DIFFRACTION (2.54 Å)