6XL4
| EGFR(T790M/V948R) in complex with AZD9291 and DDC4002 | 分子名称: | 10-benzyl-8-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, Epidermal growth factor receptor, MAGNESIUM ION, ... | 著者 | Heppner, D.E, Beyett, T.S, Eck, M.J. | 登録日 | 2020-06-28 | 公開日 | 2021-06-30 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.06 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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6XR7
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6XRG
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6Y23
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6YI8
| HUMAN FGFR4 KINASE DOMAIN (447-753) IN COMPLEX WITH ROBLITINIB | 分子名称: | Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-methanoyl-6-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide, SULFATE ION | 著者 | Ostermann, N. | 登録日 | 2020-04-01 | 公開日 | 2020-09-30 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2.13 Å) | 主引用文献 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J.Med.Chem., 63, 2020
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6YR9
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6YQ1
| FOCAL ADHESION KINASE CATALYTIC DOMAIN IN COMPLEX WITH N-Methyl-N-(3-{[2-(2-oxo-1,2,3,4-tetrahydro-quinolin-6-ylamino)-5-trifluoromethyl-pyrimidin-4-ylamino]-methyl}-pyridin-2-yl)-methanesulfonamide | 分子名称: | Focal adhesion kinase 1, SODIUM ION, SULFATE ION, ... | 著者 | Musil, D, Heinrich, T, Amaral, M. | 登録日 | 2020-04-16 | 公開日 | 2021-02-10 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (1.784 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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6YOJ
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6Z4B
| Crystal Structure of EGFR-T790M/V948R in Complex with Osimertinib and EAI045 | 分子名称: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, SULFATE ION, ... | 著者 | Niggenaber, J, Mueller, M.P, Rauh, D. | 登録日 | 2020-05-25 | 公開日 | 2020-11-11 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands. Acs Med.Chem.Lett., 11, 2020
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6Z4D
| Crystal Structure of EGFR-T790M/V948R in Complex with Mavelertinib and EAI001 | 分子名称: | (2R)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-2-phenyl-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, N-[(3R,4R)-4-fluoro-1-{6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl}pyrrolidin-3-yl]propanamide, ... | 著者 | Niggenaber, J, Mueller, M.P, Rauh, D. | 登録日 | 2020-05-25 | 公開日 | 2020-11-11 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands. Acs Med.Chem.Lett., 11, 2020
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6Z36
| Crystal structure of the ACVR1 (ALK2) kinase in complex with the compound M4K2118 | 分子名称: | 1,2-ETHANEDIOL, 4-methyl-3-(4-piperidin-4-ylphenyl)-5-(3,4,5-trimethoxyphenyl)pyridine, AMMONIUM ION, ... | 著者 | Adamson, R.J, Williams, E.P, Smil, D, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A.N. | 登録日 | 2020-05-19 | 公開日 | 2020-05-27 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (1.37 Å) | 主引用文献 | Crystal structure of the ACVR1 (ALK2) kinase in complex with the compound M4K2118 To Be Published
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6ZGC
| Crystal structure of the ACVR1 (ALK2) kinase in complex with the compound Saracatinib (AZD0530) | 分子名称: | Activin receptor type I, N-(5-CHLORO-1,3-BENZODIOXOL-4-YL)-7-[2-(4-METHYLPIPERAZIN-1-YL)ETHOXY]-5-(TETRAHYDRO-2H-PYRAN-4-YLOXY)QUINAZOLIN-4-AMINE, PHOSPHATE ION, ... | 著者 | Williams, E.P, Galan Bartual, S, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A.N. | 登録日 | 2020-06-18 | 公開日 | 2020-07-29 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2.67 Å) | 主引用文献 | Saracatinib is an efficacious clinical candidate for fibrodysplasia ossificans progressiva. JCI Insight, 6, 2021
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3I5N
| Crystal structure of c-Met with triazolopyridazine inhibitor 13 | 分子名称: | 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine, Hepatocyte growth factor receptor | 著者 | Bellon, S.F, Whittington, D.A, Long, A.M, Boezio, A.A. | 登録日 | 2009-07-06 | 公開日 | 2010-01-12 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors Bioorg.Med.Chem.Lett., 19, 2009
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3IKA
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4UYA
| Structure of MLK4 kinase domain with ATPgammaS | 分子名称: | MAGNESIUM ION, MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE MLK4, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER | 著者 | Read, J.A, Brassington, C, Pollard, H.K, Phillips, C, Green, I, Overmann, R, Collier, M. | 登録日 | 2014-08-29 | 公開日 | 2015-09-30 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | Recurrent Mlk4 Loss-of-Function Mutations Suppress Jnk Signaling to Promote Colon Tumorigenesis. Cancer Res., 76, 2016
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3II5
| The Complex of wild-type B-RAF with Pyrazolo pyrimidine inhibitor | 分子名称: | B-Raf proto-oncogene serine/threonine-protein kinase, N-[3-(3-{4-[(dimethylamino)methyl]phenyl}pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-3-(trifluoromethyl)benzamide, PHOSPHATE ION | 著者 | Xu, W, Breger, D, Torres, N, Dutia, M, Powell, D, Ciszewski, G. | 登録日 | 2009-07-31 | 公開日 | 2009-11-10 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2.79 Å) | 主引用文献 | Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. Bioorg.Med.Chem.Lett., 19, 2009
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4WD5
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3IO7
| 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2 | 分子名称: | (3S)-1-[6-(2-aminopyrazolo[1,5-a]pyrimidin-3-yl)pyrimidin-4-yl]-N,N-diethylpiperidine-3-carboxamide, Tyrosine-protein kinase JAK2 | 著者 | Zuccola, H.J, Ledeboer, M.W, Pierce, A.C. | 登録日 | 2009-08-13 | 公開日 | 2009-11-10 | 最終更新日 | 2024-03-13 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2. Bioorg.Med.Chem.Lett., 19, 2009
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4WA9
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4UWB
| Fibroblast growth factor receptor 1 kinase in complex with JK-P5 | 分子名称: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... | 著者 | Beeston, H, Tucker, J, Kankanala, J. | 登録日 | 2014-08-11 | 公開日 | 2015-09-02 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.31 Å) | 主引用文献 | Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase. Rapid Commun Mass Spectrom, 2021
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4UWC
| Fibroblast growth factor receptor 1 kinase in complex with JK-P3 | 分子名称: | 1,2-ETHANEDIOL, 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ... | 著者 | Beeston, H, Tucker, J, Kankanala, J. | 登録日 | 2014-08-11 | 公開日 | 2015-09-02 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (1.96 Å) | 主引用文献 | Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase. Rapid Commun Mass Spectrom, 2021
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3IK3
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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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7KPL
| Crystal structure of hEphB1 in apo form | 分子名称: | Ephrin type-B receptor 1 | 著者 | Ahmed, M, Wang, P, Sadek, H. | 登録日 | 2020-11-11 | 公開日 | 2021-03-10 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.705 Å) | 主引用文献 | Identification of tetracycline combinations as EphB1 tyrosine kinase inhibitors for treatment of neuropathic pain. Proc.Natl.Acad.Sci.USA, 118, 2021
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7KPM
| Crystal structure of hEphB1 bound with ADP | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Ephrin type-B receptor 1 | 著者 | Ahmed, M, Wang, P, Sadek, H. | 登録日 | 2020-11-11 | 公開日 | 2021-03-10 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (1.608 Å) | 主引用文献 | Identification of tetracycline combinations as EphB1 tyrosine kinase inhibitors for treatment of neuropathic pain. Proc.Natl.Acad.Sci.USA, 118, 2021
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