4RX8
 
 | | SYK Catalytic Domain Complexed with a Potent Triazine Inhibitor2 | | 分子名称: | 3-{[(1R,2S)-2-aminocyclohexyl]amino}-5-(1H-indol-7-ylamino)-1,2,4-triazine-6-carboxamide, GLYCEROL, Tyrosine-protein kinase SYK | | 著者 | Lee, C.C. | | 登録日 | 2014-12-09 | | 公開日 | 2015-03-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.59 Å) | | 主引用文献 | Discovery and profiling of a selective and efficacious syk inhibitor.
J.Med.Chem., 58, 2015
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4TT7
 | | Crystal structure of human ALK with a covalent modification | | 分子名称: | 1,2-ETHANEDIOL, 1-THIOETHANESULFONIC ACID, ALK tyrosine kinase receptor | | 著者 | Badger, J, Sridhar, V, Chie-Leon, B, Nienaber, V.L, Hausheer, F.H. | | 登録日 | 2014-06-19 | | 公開日 | 2015-02-11 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Novel covalent modification of human anaplastic lymphoma kinase (ALK) and potentiation of crizotinib-mediated inhibition of ALK activity by BNP7787.
Onco Targets Ther, 8, 2015
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4RMZ
 | | Crystal Structure of IRAK-4 | | 分子名称: | 3-nitro-N-[1-phenyl-5-(piperidin-1-ylmethyl)-1H-benzimidazol-2-yl]benzamide, Interleukin-1 receptor-associated kinase 4 | | 著者 | Johnstone, S, Sudom, A, Liu, J, Walker, N.P, Wang, Z. | | 登録日 | 2014-10-22 | | 公開日 | 2016-01-13 | | 最終更新日 | 2016-03-23 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Crystal structures of IRAK-4 kinase in complex with inhibitors: a serine/threonine kinase with tyrosine as a gatekeeper
To be Published
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4RX7
 | | SYK Catalytic Domain Complexed with a Potent Triazine Inhibitor | | 分子名称: | 3-{[(1R,2S)-2-aminocyclohexyl]amino}-5-{[3-(2H-1,2,3-triazol-2-yl)phenyl]amino}-1,2,4-triazine-6-carboxamide, FORMIC ACID, GLYCEROL, ... | | 著者 | Lee, C.C. | | 登録日 | 2014-12-09 | | 公開日 | 2015-03-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Discovery and profiling of a selective and efficacious syk inhibitor.
J.Med.Chem., 58, 2015
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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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4RX9
 | | SYK Catalytic Domain Complexed with a Potent Pyrimidine Inhibitor | | 分子名称: | 2-{[(1R,2S)-2-aminocyclohexyl]amino}-4-{[3-(2H-1,2,3-triazol-2-yl)phenyl]amino}pyrimidine-5-carboxamide, GLYCEROL, Tyrosine-protein kinase SYK | | 著者 | Lee, C.C. | | 登録日 | 2014-12-09 | | 公開日 | 2015-03-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Discovery and profiling of a selective and efficacious syk inhibitor.
J.Med.Chem., 58, 2015
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4WD5
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4WA9
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4RWK
 | | Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M) in complex with N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE (AZD4547) | | 分子名称: | Fibroblast growth factor receptor 1, MAGNESIUM ION, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide | | 著者 | Sohl, C.D, Anderson, K.S. | | 登録日 | 2014-12-04 | | 公開日 | 2015-04-15 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.982 Å) | | 主引用文献 | Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy.
Acs Chem.Biol., 10, 2015
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4RX5
 | | Bruton's tyrosine kinase (BTK) with pyridazinone compound 23 | | 分子名称: | 2-(2-METHOXYETHOXY)ETHANOL, GLYCEROL, N-(6-fluoro-2-methyl-3-{5-[(5-methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1,6-dihydropyridazin-3-yl}phenyl)-1-benzothiophene-2-carboxamide, ... | | 著者 | Eigenbrot, C, Yu, C. | | 登録日 | 2014-12-08 | | 公開日 | 2015-12-02 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.356 Å) | | 主引用文献 | Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.
Bioorg.Med.Chem.Lett., 26, 2016
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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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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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4RWJ
 | | Crystal Structure of FGFR1 (C488A, C584S) in complex with AZD4547 (N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE) | | 分子名称: | Fibroblast growth factor receptor 1, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide | | 著者 | Sohl, C.D, Anderson, K.S. | | 登録日 | 2014-12-04 | | 公開日 | 2015-04-22 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.489 Å) | | 主引用文献 | Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy.
Acs Chem.Biol., 10, 2015
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4V01
 | | FGFR1 in complex with ponatinib (co-crystallisation). | | 分子名称: | 1,2-ETHANEDIOL, 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 1 (FMS-RELATED TYROSINE KINASE 2, ... | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-09-10 | | 公開日 | 2014-12-10 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.33 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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4RZV
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4TRL
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4TPT
 | | Crystal Structure of the Human LIMK2 Kinase Domain In Complex With a Non-ATP Competitive Inhibitor | | 分子名称: | LIM domain kinase 2, N-{4-[(1S)-1,2-dihydroxyethyl]benzyl}-N-methyl-4-(phenylsulfamoyl)benzamide | | 著者 | Goodwin, N.C, Cianchetta, G, Hamman, B.L, Burgoon, H.A, Healy, J, Mabon, S, Strobel, E.D, Wang, S, Rawlins, D.B. | | 登録日 | 2014-06-09 | | 公開日 | 2014-10-22 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Acs Med.Chem.Lett., 6, 2015
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4RSS
 | | Crystal structure of tyrosine-protein kinase SYK with an inhibitor | | 分子名称: | 1-[(3-methyl-1-{2-[(1,2,3-trimethyl-1H-indol-5-yl)amino]pyrimidin-4-yl}-1H-pyrazol-4-yl)methyl]azetidin-3-ol, Tyrosine-protein kinase SYK | | 著者 | Lee, B.I, Lee, S.J, Choi, J.-S. | | 登録日 | 2014-11-11 | | 公開日 | 2015-10-21 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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4RT7
 | | Crystal Structure of FLT3 with a small molecule inhibitor | | 分子名称: | 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-(4-{7-[2-(morpholin-4-yl)ethoxy]imidazo[2,1-b][1,3]benzothiazol-2-yl}phenyl)urea, Receptor-type tyrosine-protein kinase FLT3 | | 著者 | Zhang, Y, Zhang, C. | | 登録日 | 2014-11-13 | | 公開日 | 2015-04-22 | | 最終更新日 | 2015-06-17 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397.
Cancer Discov, 5, 2015
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4WKQ
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4RZW
 | | Crystal structure of BRAF (R509H) kinase domain bound to AZ628 | | 分子名称: | 3-(2-cyanopropan-2-yl)-N-{4-methyl-3-[(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}benzamide, Serine/threonine-protein kinase B-raf | | 著者 | Wu, Y, Gavathiotis, E. | | 登録日 | 2014-12-24 | | 公開日 | 2016-08-10 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.493 Å) | | 主引用文献 | An integrated model of RAF inhibitor action predicts
inhibitor activity against oncogenic BRAF signaling
Cancer Cell, 30, 2016
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4RWI
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4WOV
 | | CRYSTAL STRUCTURE OF TYROSINE KINASE 2 JH2 (PSEUDO KINASE DOMAIN) COMPLEXED WITH BMS-066 AKA 2-METHOXY-N-({6-[3-METHYL-7-(METHYLAMINO)-3,5,8,10-TETRAAZATRICYCLO[7.3.0.0, 6]DODECA-1(9),2(6),4,7,11-PENTAEN-11-YL]PYRIDIN-2-YL}METHY L)ACETAMIDE | | 分子名称: | 2-methoxy-N-({6-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]pyridin-2-yl}methyl)acetamide, Non-receptor tyrosine-protein kinase TYK2, SULFATE ION | | 著者 | Muckelbauer, J.K. | | 登録日 | 2014-10-16 | | 公開日 | 2015-03-18 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain.
J.Biol.Chem., 290, 2015
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4TYE
 | | Structural analysis of the human Fibroblast Growth Factor Receptor 4 Kinase | | 分子名称: | Fibroblast growth factor receptor 4, PHOSPHATE ION | | 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 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.8 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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