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3I5N
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CRYSTAL STRUCTURE OF C-MET WITH TRIAZOLOPYRIDAZINE INHIBITOR 13
Descriptor:Hepatocyte growth factor receptor, 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine
Authors:Bellon, S.F., Whittington, D.A., Long, A.M., Boezio, A.A.
Deposit date:2009-07-06
Release date:2010-01-12
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2 Å)
Cite:Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors
Bioorg.Med.Chem.Lett., 19, 2009
5EYC
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CRYSTAL STRUCTURE OF C-MET IN COMPLEX WITH NAPHTHYRIDINONE INHIBITOR 5
Descriptor:Hepatocyte growth factor receptor, 6-[(1~{R})-1-[8-fluoranyl-6-(3-methyl-1,2-oxazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-1,6-naphthyridin-5-one
Authors:Whittington, D.A., Long, A.M.
Deposit date:2015-11-24
Release date:2016-02-10
Last modified:2016-04-06
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
J.Med.Chem., 59, 2016
5EYD
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CRYSTAL STRUCTURE OF C-MET IN COMPLEX WITH AMG 337
Descriptor:Hepatocyte growth factor receptor, 6-[(1~{R})-1-[8-fluoranyl-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-1,6-naphthyridin-5-one
Authors:Whittington, D.A., Long, A.M.
Deposit date:2015-11-24
Release date:2016-02-10
Last modified:2016-04-06
Method:X-RAY DIFFRACTION (1.85 Å)
Cite:Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
J.Med.Chem., 59, 2016
5T3Q
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CRYSTAL STRUCTURE OF THE C-MET KINASE DOMAIN IN COMPLEX WITH A PYRAZOLONE INHIBITOR
Descriptor:Hepatocyte 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
Authors:Bellon, S.F., Whittington, D.A., Long, A.M.
Deposit date:2016-08-26
Release date:2016-09-21
Method:X-RAY DIFFRACTION (2 Å)
Cite:Discovery of AMG337: Using structure guided scaffold hydridization to optimize physicochemical properties and target coverage of a MET kinase inhibitor
to be published
4FHJ
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CRYSTAL STRUCTURE OF PI3K-GAMMA IN COMPLEX WITH IMIDAZOPYRIDINE 2
Descriptor:Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(1H-pyrazol-5-yl)imidazo[1,2-a]pyridin-2-amine
Authors:Shaffer, P.L., Tang, J., Yakowec, P.
Deposit date:2012-06-06
Release date:2012-07-18
Last modified:2017-11-15
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
4FHK
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CRYSTAL STRUCTURE OF PI3K-GAMMA IN COMPLEX WITH IMIDAZOPYRIDAZINE 19E
Descriptor:Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 3-[2-methyl-6-(pyrazin-2-ylamino)pyrimidin-4-yl]-N-(1H-pyrazol-3-yl)imidazo[1,2-b]pyridazin-2-amine
Authors:Shaffer, P.L., Tang, J., Yakowec, P.
Deposit date:2012-06-06
Release date:2013-04-10
Last modified:2017-11-15
Method:X-RAY DIFFRACTION (3 Å)
Cite:Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
3CCN
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X-RAY STRUCTURE OF C-MET WITH TRIAZOLOPYRIDAZINE INHIBITOR.
Descriptor:Hepatocyte growth factor receptor, 4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]phenol
Authors:Abrecht, B.K., Harmange, J.-C., Bauer, D., Dussault, I., long, A., Bellon, S.F.
Deposit date:2008-02-26
Release date:2008-04-29
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase.
J.Med.Chem., 51, 2008
3CD8
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X-RAY STRUCTURE OF C-MET WITH TRIAZOLOPYRIDAZINE INHIBITOR.
Descriptor:Hepatocyte growth factor receptor, 7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
Authors:Bellon, S.F., Albrecht, B.K., Harmange, J.-C., Bauer, D., Choquette, D., Dussault, I.
Deposit date:2008-02-26
Release date:2008-04-29
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2 Å)
Cite:Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase.
J.Med.Chem., 51, 2008
3QAQ
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CRYSTAL STRUCTURE OF PI3K-GAMMA IN COMPLEX WITH TRIAZINE-BENZIMIDAZOLE 1
Descriptor:Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, [(4-{2-[(3-hydroxyphenyl)amino]-1H-benzimidazol-1-yl}-1,3,5-triazin-2-yl)amino]acetonitrile
Authors:Whittington, D.A., Tang, J., Yakowec, P.
Deposit date:2011-01-11
Release date:2011-03-30
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Bioorg.Med.Chem.Lett., 21, 2011
3QAR
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CRYSTAL STRUCTURE OF PI3K-GAMMA IN COMPLEX WITH TRIAZINE-BENZIMIDAZOLE 32
Descriptor:Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 1-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(1H-pyrazol-3-yl)-1H-benzimidazol-2-amine
Authors:Whittington, D.A., Tang, J., Yakowec, P.
Deposit date:2011-01-11
Release date:2011-03-30
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.65 Å)
Cite:Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Bioorg.Med.Chem.Lett., 21, 2011
4DEG
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CRYSTAL STRUCTURE OF C-MET IN COMPLEX WITH TRIAZOLOPYRIDAZINE INHIBITOR 2
Descriptor:Hepatocyte growth factor receptor, 7-methoxy-N-{[6-(3-methyl-1,2-thiazol-5-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}-1,5-naphthyridin-4-amine
Authors:Whittington, D.A., Bellon, S.F., Long, A.M.
Deposit date:2012-01-20
Release date:2012-05-30
Last modified:2012-06-20
Method:X-RAY DIFFRACTION (2 Å)
Cite:Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
4DEH
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CRYSTAL STRUCTURE OF C-MET IN COMPLEX WITH TRIAZOLOPYRIDINONE INHIBITOR 3
Descriptor:Hepatocyte growth factor receptor, 5-phenyl-3-(quinolin-6-ylmethyl)-3,5,6,7-tetrahydro-4H-[1,2,3]triazolo[4,5-c]pyridin-4-one
Authors:Whittington, D.A., Bellon, S.F., Long, A.M.
Deposit date:2012-01-20
Release date:2012-05-30
Last modified:2012-06-20
Method:X-RAY DIFFRACTION (2 Å)
Cite:Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
4DEI
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CRYSTAL STRUCTURE OF C-MET IN COMPLEX WITH TRIAZOLOPYRIDINONE INHIBITOR 24
Descriptor:Hepatocyte growth factor receptor, 3-{(1S)-1-[3-(2-methoxyethoxy)quinolin-6-yl]ethyl}-5-(3-methyl-1,2-thiazol-5-yl)-3,5-dihydro-4H-[1,2,3]triazolo[4,5-c]pyridin-4-one
Authors:Whittington, D.A., Long, A.M.
Deposit date:2012-01-20
Release date:2012-05-30
Last modified:2012-06-20
Method:X-RAY DIFFRACTION (2.05 Å)
Cite:Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012