2WD1

Human c-Met Kinase in complex with azaindole inhibitor

Summary for 2WD1

• Entry DOI: 10.2210/pdb2wd1/pdb
• Related: 1FYR 1R0P 1R1W 1SHY 1SSL 1UX3 2CEW 2G15 2UZX 2UZY
• Descriptor: HEPATOCYTE GROWTH FACTOR RECEPTOR, 1-[(2-NITROPHENYL)SULFONYL]-1H-PYRROLO[3,2-B]PYRIDINE-6-CARBOXAMIDE, GAMMA-BUTYROLACTONE, ... (4 entities in total)
• Functional Keywords: human kinase, c-met, azaindole, inhibitor, transferase, kinase, nucleotide-binding, atp-binding, tyrosine-protein kinase
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Membrane; Single-pass type I membrane protein: P08581
• Total number of polymer chains: 1
• Total formula weight: 33566.92

Authors

Porter, J.,Lumb, S.,Franklin, R.J.,Gascon-Simorte, J.M.,Calmiano, M.,Le Riche, K.,Lallemand, B.,Keyaerts, J.,Edwards, H.,Maloney, A.,Delgado, J.,King, L.,Foley, A.,Lecomte, F.,Reuberson, J.,Meier, C.,Batchelor, M. (deposition date: 2009-03-19, release date: 2009-04-28, Last modification date: 2024-05-08)

Primary citation

Porter, J.,Lumb, S.,Franklin, R.J.,Gascon-Simorte, J.M.,Calmiano, M.,Riche, K.L.,Lallemand, B.,Keyaerts, J.,Edwards, H.,Maloney, A.,Delgado, J.,King, L.,Foley, A.,Lecomte, F.,Reuberson, J.,Meier, C.,Batchelor, M.
Discovery of 4-Azaindoles as Novel Inhibitors of C- met Kinase.
Bioorg.Med.Chem.Lett., 19:2780-, 2009

PubMed Abstract: A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.

PubMed: 19369077
DOI: 10.1016/J.BMCL.2009.03.110

Experimental method

X-RAY DIFFRACTION (2 Å)