3CD8
| X-ray Structure of c-Met with triazolopyridazine Inhibitor. | Descriptor: | 7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline, Hepatocyte growth factor receptor | 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: | 2023-08-30 | 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
|
|
5EYC
| Crystal structure of c-Met in complex with naphthyridinone inhibitor 5 | Descriptor: | 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, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Long, A.M. | Deposit date: | 2015-11-24 | Release date: | 2016-02-10 | Last modified: | 2023-09-27 | 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
| Crystal structure of c-Met in complex with AMG 337 | Descriptor: | 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, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Long, A.M. | Deposit date: | 2015-11-24 | Release date: | 2016-02-10 | Last modified: | 2023-09-27 | 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
|
|
4XMO
| Crystal structure of c-Met in complex with (R)-5-(8-fluoro-3-(1-fluoro-1-(3-methoxyquinolin-6-yl)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-methylisoxazole | Descriptor: | 6-{(1R)-1-fluoro-1-[8-fluoro-6-(3-methyl-1,2-oxazol-5-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-methoxyquinoline, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Long, A.M. | Deposit date: | 2015-01-14 | Release date: | 2015-03-11 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors. J.Med.Chem., 58, 2015
|
|
4XYF
| Crystal structure of c-Met in complex with (S)-5-(8-fluoro-3-(1-(3-(2-methoxyethoxy)quinolin-6-yl)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-methylisoxazole | Descriptor: | 6-{(1S)-1-[8-fluoro-6-(3-methyl-1,2-oxazol-5-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)quinoline, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Long, A.M. | Deposit date: | 2015-02-02 | Release date: | 2015-03-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors. J.Med.Chem., 58, 2015
|
|
3I5N
| Crystal structure of c-Met with triazolopyridazine inhibitor 13 | Descriptor: | 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine, Hepatocyte growth factor receptor | 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: | 2023-09-06 | 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
|
|
3CCN
| X-ray structure of c-Met with triazolopyridazine inhibitor. | Descriptor: | 4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]phenol, Hepatocyte growth factor receptor | 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: | 2023-08-30 | 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
|
|
3B8R
| Crystal structure of the VEGFR2 kinase domain in complex with a naphthamide inhibitor | Descriptor: | 1,2-ETHANEDIOL, N-cyclopropyl-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide, Vascular endothelial growth factor receptor 2 | Authors: | Whittington, D.A, Long, A.M, Gu, Y, Zhao, H. | Deposit date: | 2007-11-01 | Release date: | 2008-04-01 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Evaluation of a Series of Naphthamides as Potent, Orally Active Vascular
Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitors J.Med.Chem., 51, 2008
|
|
3B8Q
| Crystal structure of the VEGFR2 kinase domain in complex with a naphthamide inhibitor | Descriptor: | N-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide, Vascular endothelial growth factor receptor 2 | Authors: | Whittington, D.A, Long, A.M, Gu, Y, Zhao, H. | Deposit date: | 2007-11-01 | Release date: | 2008-04-01 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.75 Å) | Cite: | Naphthamides as Novel and Potent Vascular Endothelial Growth Factor
Receptor Tyrosine Kinase Inhibitors: Design, Synthesis and Evaluation J.Med.Chem., 51, 2008
|
|
3BE2
| Crystal structure of the VEGFR2 kinase domain in complex with a benzamide inhibitor | Descriptor: | N-{3-[3-(DIMETHYLAMINO)PROPYL]-5-(TRIFLUOROMETHYL)PHENYL}-4-METHYL-3-[(3-PYRIMIDIN-4-YLPYRIDIN-2-YL)AMINO]BENZAMIDE, Vascular endothelial growth factor receptor 2 | Authors: | Whittington, D.A, Kim, J.L, Long, A.M, Gu, Y, Rose, P, Zhao, H. | Deposit date: | 2007-11-16 | Release date: | 2008-04-08 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation. J.Med.Chem., 51, 2008
|
|
4DEI
| Crystal structure of c-Met in complex with triazolopyridinone inhibitor 24 | Descriptor: | 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, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Long, A.M. | Deposit date: | 2012-01-20 | Release date: | 2012-05-30 | Last modified: | 2024-02-28 | 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
|
|
4DEH
| Crystal structure of c-Met in complex with triazolopyridinone inhibitor 3 | Descriptor: | 5-phenyl-3-(quinolin-6-ylmethyl)-3,5,6,7-tetrahydro-4H-[1,2,3]triazolo[4,5-c]pyridin-4-one, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Bellon, S.F, Long, A.M. | Deposit date: | 2012-01-20 | Release date: | 2012-05-30 | Last modified: | 2024-02-28 | 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
|
|
4DEG
| Crystal structure of c-Met in complex with triazolopyridazine inhibitor 2 | Descriptor: | 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, Hepatocyte growth factor receptor | Authors: | Whittington, D.A, Bellon, S.F, Long, A.M. | Deposit date: | 2012-01-20 | Release date: | 2012-05-30 | Last modified: | 2024-02-28 | 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
|
|
4FHJ
| Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2 | Descriptor: | 3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(1H-pyrazol-5-yl)imidazo[1,2-a]pyridin-2-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Shaffer, P.L, Tang, J, Yakowec, P. | Deposit date: | 2012-06-06 | Release date: | 2012-07-18 | Last modified: | 2023-09-13 | 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
| Crystal Structure of PI3K-gamma in Complex with Imidazopyridazine 19e | Descriptor: | 3-[2-methyl-6-(pyrazin-2-ylamino)pyrimidin-4-yl]-N-(1H-pyrazol-3-yl)imidazo[1,2-b]pyridazin-2-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Shaffer, P.L, Tang, J, Yakowec, P. | Deposit date: | 2012-06-06 | Release date: | 2013-04-10 | Last modified: | 2023-09-13 | 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
|
|