1XBA
 
 | | Crystal structure of apo syk tyrosine kinase domain | | 分子名称: | Tyrosine-protein kinase SYK | | 著者 | Atwell, S, Adams, J.M, Badger, J, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Nienaber, V.L, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | | 登録日 | 2004-08-30 | | 公開日 | 2004-11-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase.
J.Biol.Chem., 279, 2004
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1Y6A
 | | Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor | | 分子名称: | N-[5-(ETHYLSULFONYL)-2-METHOXYPHENYL]-5-[3-(2-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-AMINE, Vascular endothelial growth factor receptor 2 | | 著者 | Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A. | | 登録日 | 2004-12-05 | | 公開日 | 2005-06-07 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J.Med.Chem., 48, 2005
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1XBB
 | | Crystal structure of the syk tyrosine kinase domain with Gleevec | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Tyrosine-protein kinase SYK | | 著者 | Nienaber, V.L, Atwell, S, Adams, J.M, Badger, J, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | | 登録日 | 2004-08-30 | | 公開日 | 2004-11-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.57 Å) | | 主引用文献 | A Novel Mode of Gleevec Binding Is Revealed by the Structure of Spleen Tyrosine Kinase
J.Biol.Chem., 279, 2004
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1XBC
 | | Crystal structure of the syk tyrosine kinase domain with Staurosporin | | 分子名称: | STAUROSPORINE, Tyrosine-protein kinase SYK | | 著者 | Badger, J, Atwell, S, Adams, J.M, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Nienaber, V.L, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | | 登録日 | 2004-08-30 | | 公開日 | 2004-11-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase
J.Biol.Chem., 279, 2004
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1XKK
 | | EGFR kinase domain complexed with a quinazoline inhibitor- GW572016 | | 分子名称: | Epidermal growth factor receptor, N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE, PHOSPHATE ION | | 著者 | Wood, E.R, Truesdale, A.T, McDonald, O.B, Yuan, D, Hassell, A, Dickerson, S.H, Ellis, B, Pennisi, C, Horne, E, Lackey, K, Alligood, K.J, Rusnak, D.W, Gilmer, T.M, Shewchuk, L.M. | | 登録日 | 2004-09-29 | | 公開日 | 2004-12-07 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells.
Cancer Res., 64, 2004
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1YI6
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1YOJ
 | | Crystal structure of Src kinase domain | | 分子名称: | proto-oncogene tyrosine-protein kinase SRC | | 著者 | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | | 登録日 | 2005-01-27 | | 公開日 | 2006-01-27 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Crystal structures of active SRC kinase domain complexes
J.Mol.Biol., 353, 2005
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1YOL
 | | Crystal structure of Src kinase domain in complex with CGP77675 | | 分子名称: | 1-{4-[4-AMINO-5-(3-METHOXYPHENYL)-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL]BENZYL}PIPERIDIN-4-OL, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | | 登録日 | 2005-01-27 | | 公開日 | 2006-01-27 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Crystal structures of active SRC kinase domain complexes
J.Mol.Biol., 353, 2005
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1YOM
 | | Crystal structure of Src kinase domain in complex with Purvalanol A | | 分子名称: | 2-({6-[(3-CHLOROPHENYL)AMINO]-9-ISOPROPYL-9H-PURIN-2-YL}AMINO)-3-METHYLBUTAN-1-OL, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | | 登録日 | 2005-01-27 | | 公開日 | 2006-01-27 | | 最終更新日 | 2021-11-10 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Crystal structures of active SRC kinase domain complexes
J.Mol.Biol., 353, 2005
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1YWN
 | | Vegfr2 in complex with a novel 4-amino-furo[2,3-d]pyrimidine | | 分子名称: | N-{4-[4-AMINO-6-(4-METHOXYPHENYL)FURO[2,3-D]PYRIMIDIN-5-YL]PHENYL}-N'-[2-FLUORO-5-(TRIFLUOROMETHYL)PHENYL]UREA, Vascular endothelial growth factor receptor 2 | | 著者 | Miyazaki, Y, Matsunaga, S, Tang, J, Maeda, Y, Nakano, M, Philippe, R.J, Shibahara, M, Liu, W, Sato, H, Wang, L, Nolte, R.T. | | 登録日 | 2005-02-18 | | 公開日 | 2005-08-23 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (1.71 Å) | | 主引用文献 | Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors
Bioorg.Med.Chem.Lett., 15, 2005
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1Y6B
 | | Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor | | 分子名称: | N-(CYCLOPROPYLMETHYL)-4-(METHYLOXY)-3-({5-[3-(3-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-YL}AMINO)BENZENESULFONAMIDE, Vascular endothelial growth factor receptor 2 | | 著者 | Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A. | | 登録日 | 2004-12-05 | | 公開日 | 2005-06-07 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J.Med.Chem., 48, 2005
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1YVJ
 | | Crystal structure of the Jak3 kinase domain in complex with a staurosporine analogue | | 分子名称: | (2S,3S)-1,4-DIMERCAPTOBUTANE-2,3-DIOL, 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, Tyrosine-protein kinase JAK3 | | 著者 | Boggon, T.J, Li, Y, Manley, P.W, Eck, M.J. | | 登録日 | 2005-02-15 | | 公開日 | 2005-05-24 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog
Blood, 106, 2005
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3T9T
 | | Crystal structure of BTK mutant (F435T,K596R) complexed with Imidazo[1,5-a]quinoxaline | | 分子名称: | (2Z)-4-(dimethylamino)-N-{7-fluoro-4-[(2-methylphenyl)amino]imidazo[1,5-a]quinoxalin-8-yl}-N-methylbut-2-enamide, GLYCEROL, Tyrosine-protein kinase ITK/TSK | | 著者 | Han, S, Caspers, N. | | 登録日 | 2011-08-03 | | 公開日 | 2011-10-12 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Bioorg.Med.Chem.Lett., 21, 2011
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3TCP
 | | Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC569 | | 分子名称: | 1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, CALCIUM ION, CHLORIDE ION, ... | | 著者 | Liu, J, Yang, C, Simpson, C, DeRyckere, D, Van Deusen, A, Miley, M, Kireev, D.B, Norris-Drouin, J, Sather, S, Hunter, D, Patel, H.S, Janzen, W.P, Machius, M, Johnson, G, Earp, H.S, Graham, D.K, Frye, S, Wang, X. | | 登録日 | 2011-08-09 | | 公開日 | 2012-06-20 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.69 Å) | | 主引用文献 | Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
ACS Med Chem Lett, 3, 2012
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1MQB
 | | Crystal Structure of Ephrin A2 (ephA2) Receptor Protein Kinase | | 分子名称: | Ephrin type-A receptor 2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | 著者 | Nowakowski, J, Cronin, C.N, McRee, D.E, Knuth, M.W, Nelson, C, Pavletich, N, Rogers, J, Sang, B.C, Scheibe, D.N, Swanson, R.V, Thompson, D.A. | | 登録日 | 2002-09-16 | | 公開日 | 2003-09-16 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Structures of the Cancer Related Aurora-A, FAK and EphA2 Protein Kinases from Nanovolume Crystallography
Structure, 10, 2003
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3U6J
 | | Crystal structure of the VEGFR2 kinase domain in complex with a pyrazolone inhibitor | | 分子名称: | N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide, Vascular endothelial growth factor receptor 2 | | 著者 | Whittington, D.A, Long, A, Rose, P, Gu, Y, Zhao, H. | | 登録日 | 2011-10-12 | | 公開日 | 2012-02-22 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
J.Med.Chem., 55, 2012
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3TJC
 | | Co-crystal structure of jak2 with thienopyridine 8 | | 分子名称: | 4-amino-N-methyl-2-[4-(morpholin-4-yl)phenyl]thieno[3,2-c]pyridine-7-carboxamide, Tyrosine-protein kinase JAK2 | | 著者 | Huang, X. | | 登録日 | 2011-08-24 | | 公開日 | 2011-11-30 | | 最終更新日 | 2011-12-28 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Discovery of potent and highly selective thienopyridine janus kinase 2 inhibitors.
J.Med.Chem., 54, 2011
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3TUB
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3U6I
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3TV6
 | | Human B-Raf Kinase Domain in Complex with a Methoxypyrazolopyridinyl Benzamide Inhibitor | | 分子名称: | 2,6-difluoro-N-(3-methoxy-2H-pyrazolo[3,4-b]pyridin-5-yl)-3-[(propylsulfonyl)amino]benzamide, Serine/threonine-protein kinase B-raf | | 著者 | Voegtli, W.C, Sturgis, H.L, Wu, W.-I. | | 登録日 | 2011-09-19 | | 公開日 | 2011-10-05 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
ACS Med Chem Lett, 2, 2011
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3TZ7
 | | Kinase domain of cSrc in complex with RL103 | | 分子名称: | N-(4-{[4-({[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]carbamoyl}amino)phenyl]amino}quinazolin-6-yl)-4-(dimethylamino)butanamide, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Gruetter, C, Richters, A, Rauh, D. | | 登録日 | 2011-09-27 | | 公開日 | 2012-10-10 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Overcoming Gatekeeper Mutations in cSrc and Abl by Hybrid Compound Design
To be Published
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3U51
 | | Src in complex with DNA-templated macrocyclic inhibitor MC1 | | 分子名称: | Proto-oncogene tyrosine-protein kinase Src, macrocyclic inhibitor MC1 | | 著者 | Seeliger, M.A, Liu, D.R, Georghiou, G, Kleiner, R.E, Pulkoski-Gross, M. | | 登録日 | 2011-10-10 | | 公開日 | 2012-02-22 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.241 Å) | | 主引用文献 | Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles.
Nat.Chem.Biol., 8, 2012
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3U6H
 | | Crystal structure of c-Met in complex with pyrazolone inhibitor 26 | | 分子名称: | Hepatocyte growth factor receptor, N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide | | 著者 | Bellon, S.F, Whittington, D.A, Long, A.L. | | 登録日 | 2011-10-12 | | 公開日 | 2012-02-22 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
J.Med.Chem., 55, 2012
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3TJD
 | | co-crystal structure of Jak2 with thienopyridine 19 | | 分子名称: | 4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide, Tyrosine-protein kinase JAK2 | | 著者 | Huang, X. | | 登録日 | 2011-08-24 | | 公開日 | 2011-11-30 | | 最終更新日 | 2011-12-28 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery of potent and highly selective thienopyridine janus kinase 2 inhibitors.
J.Med.Chem., 54, 2011
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3TUD
 | | Crystal structure of SYK kinase domain with N-(4-methyl-3-(8-methyl-7-oxo-2-(phenylamino)-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide | | 分子名称: | N-{4-methyl-3-[8-methyl-7-oxo-2-(phenylamino)-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl]phenyl}-3-(trifluoromethyl)benzamide, Tyrosine-protein kinase SYK | | 著者 | Lovering, F, McDonald, J, Whitlock, G, Glossop, P, Phillips, C, Sabnis, Y, Ryan, M, Fitz, L, Lee, J, Chang, J.S, Han, S, Kurumbail, R, Thorarenson, A. | | 登録日 | 2011-09-16 | | 公開日 | 2012-08-29 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Identification of Type-II Inhibitors Using Kinase Structures.
Chem.Biol.Drug Des., 80, 2012
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