7LL4
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7LL5
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7LG8
| EGFR (T79M/V948R) in complex with naquotinib and an allosteric inhibitor | 分子名称: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{6-[4-(1-methylpiperidin-4-yl)phenyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide, 6-ethyl-3-[[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-[(3R)-1-prop-2-enoylpyrrolidin-3-yl]oxy-pyrazin e-2-carboxamide, Epidermal growth factor receptor | 著者 | Beyett, T.S, Eck, M.J. | 登録日 | 2021-01-19 | 公開日 | 2022-02-23 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.93 Å) | 主引用文献 | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nat Commun, 13, 2022
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7LTX
| EGFR (T790M/V948R) in complex with quinazolinone allosteric inhibitor | 分子名称: | (2R)-2-{5-fluoro-6-[4-(1-methylpiperidin-4-yl)phenyl]-4-oxoquinazolin-3(4H)-yl}-2-phenyl-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | 著者 | Beyett, T.S, Eck, M.J. | 登録日 | 2021-02-20 | 公開日 | 2022-02-23 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | 主引用文献 | Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg.Med.Chem.Lett., 68, 2022
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1FGI
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1FGK
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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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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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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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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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4U0I
| Crystal structure of KIT 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, Mast/stem cell growth factor receptor Kit,Mast/stem cell growth factor receptor Kit, PHOSPHATE ION | 著者 | Zhou, T, Zhu, X, Dalgarno, D.C. | 登録日 | 2014-07-11 | 公開日 | 2014-10-08 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Ponatinib Inhibits Polyclonal Drug-Resistant KIT Oncoproteins and Shows Therapeutic Potential in Heavily Pretreated Gastrointestinal Stromal Tumor (GIST) Patients. Clin.Cancer Res., 20, 2014
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2XIR
| Crystal structure of the VEGFR2 kinase domain in complex with PF- 00337210 (N,2-dimethyl-6-(7-(2-morpholinoethoxy)quinolin-4-yloxy) benzofuran-3-carboxamide) | 分子名称: | N,2-DIMETHYL-6-{[7-(2-MORPHOLIN-4-YLETHOXY)QUINOLIN-4-YL]OXY}-1-BENZOFURAN-3-CARBOXAMIDE, VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 | 著者 | McTigue, M, Wickersham, J, Pinko, C, Hong, Y, Marrone, T. | 登録日 | 2010-06-30 | 公開日 | 2011-04-13 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | 主引用文献 | Discovery of the Selective Vegfr Inhibitor Pf- 00337210 To be Published
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3UE4
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2XVD
| ephB4 kinase domain inhibitor complex | 分子名称: | EPHRIN TYPE-B RECEPTOR 4, MAGNESIUM ION, {4-METHYL-3-[(1-METHYLETHYL)(2-{[3-(METHYLSULFONYL)-5-MORPHOLIN-4-YLPHENYL]AMINO}PYRIMIDIN-4-YL)AMINO]PHENYL}METHANOL | 著者 | Read, J, Brassington, C.A, Green, I, McCall, E.J, Valentine, A.L. | 登録日 | 2010-10-25 | 公開日 | 2011-06-08 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | Inhibitors of the Tyrosine Kinase Ephb4. Part 4: Discovery and Optimization of a Benzylic Alcohol Series. Bioorg.Med.Chem.Lett., 21, 2011
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3ULZ
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4U5J
| C-Src in complex with Ruxolitinib | 分子名称: | (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, Proto-oncogene tyrosine-protein kinase Src | 著者 | Chen, Y, Duan, Y, Chen, L. | 登録日 | 2014-07-25 | 公開日 | 2014-09-17 | 最終更新日 | 2024-06-26 | 実験手法 | X-RAY DIFFRACTION (2.26 Å) | 主引用文献 | c-Src Binds to the Cancer Drug Ruxolitinib with an Active Conformation Plos One, 9, 2014
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3UG2
| Crystal structure of the mutated EGFR kinase domain (G719S/T790M) in complex with gefitinib | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Epidermal growth factor receptor, Gefitinib | 著者 | Parker, L.J, Handa, N, Yoshikawa, S, Kukimoto-Niino, M, Shirouzu, M, Yokoyama, S. | 登録日 | 2011-11-02 | 公開日 | 2012-03-07 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor Oncogene, 32, 2013
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3UIM
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2XYU
| Crystal structure of EphA4 kinase domain in complex with VUF 12058 | 分子名称: | 5-(5-FLUORO-2-METHYLPHENYL)-6,7,8,9-TETRAHYDRO-3H-PYRAZOLO[3,4-C]ISOQUINOLIN-1-AMINE, EPHRIN TYPE-A RECEPTOR 4,, GLYCEROL | 著者 | Farenc, C.J.A, Celie, P.H.N, vanLinden, O.P.J, Siegal, G. | 登録日 | 2010-11-19 | 公開日 | 2011-11-30 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.117 Å) | 主引用文献 | Fragment Based Lead Discovery of Small Molecule Inhibitors for the Epha4 Receptor Tyrosine Kinase. Eur.J.Med.Chem., 47, 2012
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4TYG
| Structural analysis of the human Fibroblast Growth Factor Receptor 4 Kinase | 分子名称: | ACETATE ION, Fibroblast growth factor receptor 4 | 著者 | Lesca, E, Lammens, A, Huber, R, Augustin, M. | 登録日 | 2014-07-08 | 公開日 | 2014-09-24 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Structural analysis of the human fibroblast growth factor receptor 4 kinase. J.Mol.Biol., 426, 2014
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7YBO
| Crystal structure of FGFR4 kinase domain with 10z | 分子名称: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-6-bromanyl-5-(hydroxymethyl)-1-(2-morpholin-4-ylethyl)pyrrolo[3,2-b]pyridine-3-carboxamide | 著者 | Chen, X.J, Lin, Q.M, Chen, Y.H. | 登録日 | 2022-06-29 | 公開日 | 2022-11-16 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2.307 Å) | 主引用文献 | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors. J.Med.Chem., 65, 2022
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7YC3
| Crystal structure of FGFR4 kinase domain with 10t | 分子名称: | 6-bromanyl-~{N}-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-5-methanoyl-1-(2-morpholin-4-ylethyl)pyrrolo[3,2-b]pyridine-3-carboxamide, Fibroblast growth factor receptor 4, GLYCEROL, ... | 著者 | Chen, X.J, Lin, Q.M, Chen, Y.H. | 登録日 | 2022-06-30 | 公開日 | 2022-11-16 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (1.987 Å) | 主引用文献 | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors. J.Med.Chem., 65, 2022
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2XP2
| Structure of the Human Anaplastic Lymphoma Kinase in Complex with Crizotinib (PF-02341066) | 分子名称: | 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-amine, TYROSINE-PROTEIN KINASE RECEPTOR | 著者 | McTigue, M, Deng, Y, Liu, W, Brooun, A, Timofeevski, S, Marrone, T, Cui, J.J. | 登録日 | 2010-08-24 | 公開日 | 2010-09-15 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Structure Based Drug Design of Crizotinib (Pf-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (C-met) Kinase and Anaplastic Lymphoma Kinase (Alk). J.Med.Chem, 54, 2011
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7YC1
| Crystal structure of FGFR4 kinase domain with 10d | 分子名称: | Fibroblast growth factor receptor 4, GLYCEROL, SULFATE ION, ... | 著者 | Chen, X.J, Lin, Q.M, Chen, Y.H. | 登録日 | 2022-06-30 | 公開日 | 2022-11-16 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2.535 Å) | 主引用文献 | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors. J.Med.Chem., 65, 2022
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7YBP
| Crystal structure of FGFR4(V550L) kinase domain with 10z | 分子名称: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-6-bromanyl-5-(hydroxymethyl)-1-(2-morpholin-4-ylethyl)pyrrolo[3,2-b]pyridine-3-carboxamide | 著者 | Chen, X.J, Lin, Q.M, Chen, Y.H. | 登録日 | 2022-06-29 | 公開日 | 2022-11-16 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2.243 Å) | 主引用文献 | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors. J.Med.Chem., 65, 2022
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