5T3Q

Crystal structure of the c-Met kinase domain in complex with a pyrazolone inhibitor

Summary for 5T3Q

Related3U6I
DescriptorHepatocyte growth factor receptor, N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (3 entities in total)
Functional Keywordsphosphotransferase, cancer, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationMembrane; Single-pass type I membrane protein. Isoform 3: Secreted P08581
Total number of polymer chains1
Total molecular weight35772.3
Authors
Bellon, S.F.,Whittington, D.A.,Long, A.M. (deposition date: 2016-08-26, release date: 2016-09-21)
Primary citation
Boezio, A.A.,Peterson, E.A.,Harmange, J.-C.
Discovery of AMG337: Using structure guided scaffold hydridization to optimize physicochemical properties and target coverage of a MET kinase inhibitor
to be published,
Experimental method
X-RAY DIFFRACTION (2 Å)
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Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers0.249302.8%6.1%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution

More Asymmetric unit images

Molmil generated image of 5t3q
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Molmil generated image of 5t3q
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Molmil generated image of 5t3q
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More Biological unit images

Molmil generated image of 5t3q
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Molmil generated image of 5t3q
rotated about x axis by 90°
Molmil generated image of 5t3q
rotated about y axis by 90°
(*)In the case of coarse surface representation, the asymmetric unit is shown as red ribbon representation.
Coordinate files for Biological unit (5t3q.pdb1.gz [99.98 KB])