2OO8
 
 | | Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors | | Descriptor: | Angiopoietin-1 receptor, N-{3-[3-(DIMETHYLAMINO)PROPYL]-5-(TRIFLUOROMETHYL)PHENYL}-4-METHYL-3-[(3-PYRIMIDIN-4-YLPYRIDIN-2-YL)AMINO]BENZAMIDE | | Authors: | Bellon, S.F, Kim, J. | | Deposit date: | 2007-01-25 | | Release date: | 2007-03-20 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Bioorg.Med.Chem.Lett., 17, 2007
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2P2I
 | | Crystal structure of the VEGFR2 kinase domain in complex with a nicotinamide inhibitor | | Descriptor: | N-(4-phenoxyphenyl)-2-[(pyridin-4-ylmethyl)amino]nicotinamide, Vascular endothelial growth factor receptor 2 | | Authors: | Whittington, D.A, Kim, J.L, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | Deposit date: | 2007-03-07 | | Release date: | 2007-03-20 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor
J.Med.Chem., 50, 2007
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2P0C
 | | Catalytic Domain of the Proto-oncogene Tyrosine-protein Kinase MER | | Descriptor: | BETA-MERCAPTOETHANOL, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Walker, J.R, Huang, X, Finerty Jr, P.J, Weigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2007-02-28 | | Release date: | 2007-05-08 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structural insights into the inhibited states of the Mer receptor tyrosine kinase.
J.Struct.Biol., 165, 2009
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2PWL
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2PVF
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2PL0
 | | LCK bound to imatinib | | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Proto-oncogene tyrosine-protein kinase LCK | | Authors: | Jacobs, M.D. | | Deposit date: | 2007-04-18 | | Release date: | 2007-10-09 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Classifying protein kinase structures guides use of ligand-selectivity profiles to predict inactive conformations: Structure of lck/imatinib complex.
Proteins, 70, 2007
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2PZ5
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2OIB
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2NRY
 | | Crystal structure of IRAK-4 | | Descriptor: | STAUROSPORINE, interleukin-1 receptor-associated kinase 4 | | Authors: | Wang, Z, Liu, J, Walker, N.P.C. | | Deposit date: | 2006-11-02 | | Release date: | 2006-12-12 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Crystal structures of IRAK-4 kinase in complex with inhibitors: a serine/threonine kinase with tyrosine as a gatekeeper.
Structure, 14, 2006
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2PSQ
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2PVY
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2PZR
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2PY3
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2PZP
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2Q0B
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2R2P
 | | Kinase domain of human ephrin type-A receptor 5 (EphA5) | | Descriptor: | CHLORIDE ION, Ephrin type-A receptor 5, SULFATE ION | | Authors: | Walker, J.R, Cuerrier, D, Butler-Cole, C, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2007-08-27 | | Release date: | 2007-09-25 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Kinase Domain of Human Ephrin Type-A Receptor 5 (EphA5).
To be Published
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3L8P
 | | Crystal structure of cytoplasmic kinase domain of Tie2 complexed with inhibitor CEP11207 | | Descriptor: | 2-methyl-11-(1-methylethyl)-8-[(2S)-tetrahydro-2H-pyran-2-yl]-2,11,12,13-tetrahydro-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one, Angiopoietin-1 receptor | | Authors: | Fedorov, A.A, Fedorov, E.V, Pauletti, D, Meyer, S.L, Hudkins, R.L, Almo, S.C. | | Deposit date: | 2010-01-03 | | Release date: | 2010-10-06 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Crystal structure of cytoplasmic kinase domain of Tie2 complexed with inhibitor CEP11207
To be Published
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3LCT
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3LMG
 | | Crystal structure of the ERBB3 kinase domain in complex with AMP-PNP | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Receptor tyrosine-protein kinase erbB-3 | | Authors: | Shi, F, Lemmon, M.A. | | Deposit date: | 2010-01-30 | | Release date: | 2010-04-21 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation.
Proc.Natl.Acad.Sci.USA, 107, 2010
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3LOK
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3LPB
 | | Crystal structure of Jak2 complexed with a potent 2,8-diaryl-quinoxaline inhibitor | | Descriptor: | N-methyl-4-[3-(3,4,5-trimethoxyphenyl)quinoxalin-5-yl]benzenesulfonamide, Tyrosine-protein kinase JAK2 | | Authors: | Tavares, G.A, Pissot-Soldermann, C, Gerspacher, M, Furet, P, Kroemer, M. | | Deposit date: | 2010-02-05 | | Release date: | 2010-04-28 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors
Bioorg.Med.Chem.Lett., 20, 2010
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3L8V
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3L9P
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7LL5
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7LTZ
 | | Bruton's tyrosine kinase in complex with compound 51 | | Descriptor: | 1-~{tert}-butyl-~{N}-[(5~{R})-8-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-2-(oxetan-3-yl)-1,3,4,5-tetrahydro-2-benzazepin-5-yl]-1,2,3-triazole-4-carboxamide, 2,3-DIHYDROXY-1,4-DITHIOBUTANE, ACETATE ION, ... | | Authors: | Metrick, C.M, Marcotte, D.J. | | Deposit date: | 2021-02-20 | | Release date: | 2022-01-12 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.53 Å) | | Cite: | Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
J.Med.Chem., 65, 2022
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