6Q7B
 
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with the NVP-BHG712 derivative ATDL09 | | 分子名称: | 3-[[4-imidazol-1-yl-6-[(3~{S})-3-oxidanylpyrrolidin-1-yl]-1,3,5-triazin-2-yl]amino]-4-methyl-~{N}-[3-(trifluoromethyl)phenyl]benzamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Troester, A, Witt, K, Linhard, V.L, Gande, S.L, Saxena, K, Schwalbe, H. | | 登録日 | 2018-12-13 | | 公開日 | 2020-01-15 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.009 Å) | | 主引用文献 | Effects of NVP-BHG712 chemical modifications on EPHA2 binding and affinity
To Be Published
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4UXL
 | | Structure of Human ROS1 Kinase Domain in Complex with PF-06463922 | | 分子名称: | (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS | | 著者 | McTigue, M, Deng, Y, Liu, W, Brooun, A, Stewart, A. | | 登録日 | 2014-08-25 | | 公開日 | 2015-03-11 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Pf-06463922 is a Potent and Selective Next-Generation Ros1/Alk Inhibitor Capable of Blocking Crizotinib-Resistant Ros1 Mutations.
Proc.Natl.Acad.Sci.USA, 112, 2015
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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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3HGK
 | | crystal structure of effect protein AvrptoB complexed with kinase Pto | | 分子名称: | Effector protein hopAB2, Protein kinase | | 著者 | Dong, J, Fan, F, Gu, L, Chai, J. | | 登録日 | 2009-05-14 | | 公開日 | 2009-06-23 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Crystal Structure of the Complex between Pseudomonas Effector AvrPtoB and the Tomato Pto Kinase Reveals Both a Shared and a Unique Interface Compared with AvrPto-Pto
Plant Cell, 21, 2009
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4NWM
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4O2P
 | | Kinase domain of cSrc in complex with a substituted pyrazolopyrimidine | | 分子名称: | 1-[(2R)-2-chloro-2-phenylethyl]-6-{[2-(morpholin-4-yl)ethyl]sulfanyl}-N-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Richters, A, Rauh, D. | | 登録日 | 2013-12-17 | | 公開日 | 2015-03-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Combining X-ray Crystallography and Molecular Modeling toward the Optimization of Pyrazolo[3,4-d]pyrimidines as Potent c-Src Inhibitors Active in Vivo against Neuroblastoma.
J.Med.Chem., 58, 2015
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4UWY
 | | FGFR1 Apo structure | | 分子名称: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | | 著者 | Thiyagarajan, N, Bunney, T, Katan, M. | | 登録日 | 2014-08-15 | | 公開日 | 2015-02-25 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.305 Å) | | 主引用文献 | The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study
Ebiomedicine, 2, 2015
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4OT6
 | | Crystal structure of BTK kinase domain complexed with 4-Methanesulfonyl-N-(3-{8-[4-(morpholine-4-carbonyl)-phenylamino]-imidazo[1,2-a]pyrazin-6-yl}-phenyl)-benzamide | | 分子名称: | 4-(methylsulfonyl)-N-[3-(8-{[4-(morpholin-4-ylcarbonyl)phenyl]amino}imidazo[1,2-a]pyrazin-6-yl)phenyl]benzamide, Tyrosine-protein kinase BTK | | 著者 | Kuglstatter, A, Wong, A. | | 登録日 | 2014-02-13 | | 公開日 | 2014-05-14 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | Structure-Based Drug Design of RN486, a Potent and Selective Bruton's Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis.
J.Med.Chem., 58, 2015
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4WD5
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1AGW
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4WA9
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1BYG
 | | KINASE DOMAIN OF HUMAN C-TERMINAL SRC KINASE (CSK) IN COMPLEX WITH INHIBITOR STAUROSPORINE | | 分子名称: | PROTEIN (C-TERMINAL SRC KINASE), STAUROSPORINE | | 著者 | Antson, A.A, Lamers, M.B.A.C, Scott, R.K, Williams, D.H, Hubbard, R.E. | | 登録日 | 1998-10-14 | | 公開日 | 1999-10-14 | | 最終更新日 | 2023-08-09 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine.
J.Mol.Biol., 285, 1999
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8XZ7
 | | FGFR1 kinase domain with a covalent inhibitor 10h | | 分子名称: | 5-azanyl-3-[2-[4,6-bis(fluoranyl)-2-methyl-3~{H}-benzimidazol-5-yl]ethynyl]-1-[[3-(prop-2-enoylamino)phenyl]methyl]pyrazole-4-carboxamide, Fibroblast growth factor receptor 1, SULFATE ION | | 著者 | Chen, X.J, Chen, Y.H. | | 登録日 | 2024-01-20 | | 公開日 | 2024-06-26 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
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8ZKD
 | | The Crystal Structure of the RON from Biortus. | | 分子名称: | 1,2-ETHANEDIOL, MAGNESIUM ION, Macrophage-stimulating protein receptor beta chain, ... | | 著者 | Wang, F, Cheng, W, Yuan, Z, Qi, J, Pan, W. | | 登録日 | 2024-05-16 | | 公開日 | 2024-06-26 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | The Crystal Structure of the RON from Biortus.
To Be Published
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5D7V
 | | Crystal structure of PTK6 kinase domain | | 分子名称: | GLYCEROL, PHOSPHATE ION, Protein-tyrosine kinase 6 | | 著者 | Thakur, M.K, Birudukota, S, Swaminathan, S, Tyagi, R, Gosu, R. | | 登録日 | 2015-08-14 | | 公開日 | 2016-08-17 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Crystal structure of the kinase domain of human protein tyrosine kinase 6 (PTK6) at 2.33 angstrom resolution
Biochem.Biophys.Res.Commun., 478, 2016
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8YKI
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8Y22
 | | FGFR1 kinase domain with a covalent inhibitor 9g | | 分子名称: | Fibroblast growth factor receptor 1, SULFATE ION, ~{N}-[4-[[4-azanyl-3-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]propanamide | | 著者 | Chen, X.J, Chen, Y.H. | | 登録日 | 2024-01-25 | | 公開日 | 2024-06-26 | | 実験手法 | X-RAY DIFFRACTION (2.792 Å) | | 主引用文献 | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
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5DG5
 | | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET IN COMPLEX WITH ALTIRATINIB ANALOG DP-4157 | | 分子名称: | Hepatocyte growth factor receptor, N-(2,5-difluoro-4-{[2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxam ide | | 著者 | Smith, B.D, Kaufman, M.D, Leary, C.B, Turner, B.A, Wise, S.A, Ahn, Y.M, Booth, R.J, Caldwell, T.M, Ensinger, C.L, Hood, M.M, Lu, W.-P, Patt, T.W, Patt, W.C, Rutkoski, T.J, Samarakoon, T, Telikepalli, H, Vogeti, L, Vogeti, S, Yates, K.M, Chun, L, Stewart, L.J, Clare, M, Flynn, D.L. | | 登録日 | 2015-08-27 | | 公開日 | 2016-08-31 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2.
Mol.Cancer Ther., 14, 2015
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5D12
 | | Kinase domain of cSrc in complex with RL40 | | 分子名称: | N-[2-phenyl-4-(1H-pyrazol-3-ylamino)quinazolin-7-yl]prop-2-enamide, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Becker, C, Richters, A, Engel, J, Rauh, D. | | 登録日 | 2015-08-03 | | 公開日 | 2015-09-09 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
J.Med.Chem., 58, 2015
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6YT6
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6YXV
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6YVY
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6YVS
 | | FOCAL ADHESION KINASE CATALYTIC DOMAIN IN COMPLEX WITH 5-{4-[(Pyridin-3-ylmethyl)-amino]-5-trifluoromethyl-pyrimidin-2-ylamino}-1,3-dihydro-indol-2-one | | 分子名称: | 5-[[4-(pyridin-3-ylmethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-1,3-dihydroindol-2-one, Focal adhesion kinase 1, SULFATE ION | | 著者 | Musil, D, Heinrich, T, Amaral, M. | | 登録日 | 2020-04-28 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.81 Å) | | 主引用文献 | Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Cell Chem Biol, 28, 2021
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7REE
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7R60
 | | BTK in complex with 18A | | 分子名称: | 2-(4-phenoxyphenoxy)-5-[(3R)-1-(prop-2-enoyl)piperidin-3-yl]pyridine-3-carboxamide, Tyrosine-protein kinase BTK | | 著者 | Gardberg, A. | | 登録日 | 2021-06-22 | | 公開日 | 2021-10-06 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | | 主引用文献 | Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity.
Chemmedchem, 16, 2021
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