4V0G
| JAK3 in complex with a covalent EGFR inhibitor | 分子名称: | N-[3-(2-{3-amino-6-[1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]pyrazin-2-yl}-1H-benzimidazol-1-yl)phenyl]propanamide, TYROSINE-PROTEIN KINASE JAK3 | 著者 | Debreczeni, J.E, Hennessy, E.J, Chuaquini, C, Ashton, S, Coclough, N, Cross, D.A.E, Eberlein, C, Gingipalli, L, Klinowska, T.C.M, Orme, J.P, Sha, L, Wu, X. | 登録日 | 2014-09-16 | 公開日 | 2016-01-13 | 実験手法 | X-RAY DIFFRACTION (3 Å) | 主引用文献 | Utilisation of Structure Based Design to Identify Novel, Irreversible Inhibitors of the Epidermal Growth Factor Receptor (Egfr) Harboring the Gatekeeper T790M Mutation To be Published
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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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7NZN
| Structure of RET kinase domain bound to inhibitor JB-48 | 分子名称: | 2-[4-[[4-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-6-[(3-methyl-1~{H}-pyrazol-5-yl)amino]pyrimidin-2-yl]amino]phenyl]-~{N}-(3-fluorophenyl)ethanamide, FORMIC ACID, Proto-oncogene tyrosine-protein kinase receptor Ret | 著者 | Briggs, D.C, McDonald, N.Q. | 登録日 | 2021-03-24 | 公開日 | 2022-02-09 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.39 Å) | 主引用文献 | Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J.Med.Chem., 65, 2022
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7Z5W
| ROS1 with AstraZeneca ligand 1 | 分子名称: | Proto-oncogene tyrosine-protein kinase ROS, SULFATE ION, ~{N}-[6-methyl-2-[(2~{S})-2-[3-(3-methylpyrazin-2-yl)-1,2-oxazol-5-yl]pyrrolidin-1-yl]pyrimidin-4-yl]-1,3-thiazol-2-amine | 著者 | Hargreaves, D. | 登録日 | 2022-03-10 | 公開日 | 2022-08-17 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.254 Å) | 主引用文献 | Virtual Screening in the Cloud Identifies Potent and Selective ROS1 Kinase Inhibitors. J.Chem.Inf.Model., 62, 2022
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7Z5X
| ROS1 with AstraZeneca ligand 2 | 分子名称: | (2R)-2-[5-(6-amino-5-{(1R)-1-[2-(1,3-dihydro-2H-1,2,3-triazol-2-yl)-5-fluorophenyl]ethoxy}pyridin-3-yl)-4-methyl-1,3-thiazol-2-yl]propane-1,2-diol, Proto-oncogene tyrosine-protein kinase ROS | 著者 | Hargreaves, D. | 登録日 | 2022-03-10 | 公開日 | 2022-08-17 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.035 Å) | 主引用文献 | Virtual Screening in the Cloud Identifies Potent and Selective ROS1 Kinase Inhibitors. J.Chem.Inf.Model., 62, 2022
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4MXY
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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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4UXQ
| FGFR4 in complex with Ponatinib | 分子名称: | 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide, FIBROBLAST GROWTH FACTOR RECEPTOR 4, SULFATE ION | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | 登録日 | 2014-08-27 | 公開日 | 2014-12-03 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4 Structure, 22, 2014
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1FPU
| CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR | 分子名称: | N-[4-METHYL-3-[[4-(3-PYRIDINYL)-2-PYRIMIDINYL]AMINO]PHENYL]-3-PYRIDINECARBOXAMIDE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL | 著者 | Schindler, T, Bornmann, W, Pellicena, P, Miller, W.T, Clarkson, B, Kuriyan, J. | 登録日 | 2000-08-31 | 公開日 | 2000-09-20 | 最終更新日 | 2024-03-13 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science, 289, 2000
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4NK9
| Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 1 | 分子名称: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N~4~-{5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl}-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, ... | 著者 | Norman, R.A, Klein, T. | 登録日 | 2013-11-12 | 公開日 | 2013-12-18 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2.57 Å) | 主引用文献 | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures. ACS Med Chem Lett, 5, 2014
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1AGW
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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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6R5F
| Crystal structure of RIP1 kinase in complex with DHP77 | 分子名称: | Receptor-interacting serine/threonine-protein kinase 1, [(5~{S})-5-[3,5-bis(fluoranyl)phenyl]pyrazolidin-1-yl]-[1-(5-methyl-1,3,4-oxadiazol-2-yl)piperidin-4-yl]methanone | 著者 | Thorpe, J.H, Campobasso, N, Harris, P.A. | 登録日 | 2019-03-25 | 公開日 | 2019-05-01 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | 主引用文献 | Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase. J.Med.Chem., 62, 2019
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6RFJ
| IRAK4 IN COMPLEX WITH inhibitor | 分子名称: | Interleukin-1 receptor-associated kinase 4, SULFATE ION, methyl 4-[4-[[6-(cyanomethyl)-2-[(1-methylpyrazol-4-yl)amino]pyrido[3,2-d]pyrimidin-4-yl]amino]cyclohexyl]piperazine-1-carboxylate | 著者 | Xue, Y, Degorce, S.L, Robb, G.R, Ferguson, A.D. | 登録日 | 2019-04-15 | 公開日 | 2019-10-30 | 最終更新日 | 2019-11-27 | 実験手法 | X-RAY DIFFRACTION (2.61 Å) | 主引用文献 | Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265PMutant Diffuse Large B Cell Lymphoma. J.Med.Chem., 62, 2019
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6RLN
| Crystal structure of RIP1 kinase in complex with GSK3145095 | 分子名称: | Receptor-interacting serine/threonine-protein kinase 1, ~{N}-[(3~{S})-7,9-bis(fluoranyl)-2-oxidanylidene-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-3-(phenylmethyl)-1~{H}-1,2,4-triazole-5-carboxamide | 著者 | Thorpe, J.H, Harris, P.A. | 登録日 | 2019-05-02 | 公開日 | 2019-07-03 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2.87 Å) | 主引用文献 | Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. Acs Med.Chem.Lett., 10, 2019
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6RSE
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1FGK
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1FGI
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2G2H
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2G15
| Structural Characterization of autoinhibited c-Met kinase | 分子名称: | activated met oncogene | 著者 | Wang, W, Marimuthu, A, Tsai, J, Kumar, A, Krupka, H.I, Zhang, C, Powell, B, Suzuki, Y, Nguyen, H, Tabrizizad, M, Luu, C, West, B.L. | 登録日 | 2006-02-13 | 公開日 | 2006-03-21 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase. Proc.Natl.Acad.Sci.Usa, 103, 2006
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1GAG
| CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR | 分子名称: | BISUBSTRATE PEPTIDE INHIBITOR, INSULIN RECEPTOR, TYROSINE KINASE DOMAIN, ... | 著者 | Parang, K, Till, J.H, Ablooglu, A.J, Kohanski, R.A, Hubbard, S.R, Cole, P.A. | 登録日 | 2000-11-29 | 公開日 | 2001-01-17 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Mechanism-based design of a protein kinase inhibitor. Nat.Struct.Biol., 8, 2001
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2G2F
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1FVR
| TIE2 KINASE DOMAIN | 分子名称: | TYROSINE-PROTEIN KINASE TIE-2 | 著者 | Shewchuk, L.M, Hassell, A.M, Ellis, B, Holmes, W.D, Davis, R, Horne, E.L, Kadwell, S.H, McKee, D.D, Moore, J.T. | 登録日 | 2000-09-20 | 公開日 | 2001-09-20 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Structure of the Tie2 RTK domain: self-inhibition by the nucleotide binding loop, activation loop, and C-terminal tail. Structure Fold.Des., 8, 2000
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2G1T
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1GJO
| The FGFr2 tyrosine kinase domain | 分子名称: | FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION | 著者 | Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J. | 登録日 | 2001-07-31 | 公開日 | 2003-08-15 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | The Fgfr2 Tyrosine Kinase Domain To be Published
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