1YVJ
| Crystal structure of the Jak3 kinase domain in complex with a staurosporine analogue | Descriptor: | (2S,3S)-1,4-DIMERCAPTOBUTANE-2,3-DIOL, 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, Tyrosine-protein kinase JAK3 | Authors: | Boggon, T.J, Li, Y, Manley, P.W, Eck, M.J. | Deposit date: | 2005-02-15 | Release date: | 2005-05-24 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog Blood, 106, 2005
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2F4J
| Structure of the Kinase Domain of an Imatinib-Resistant Abl Mutant in Complex with the Aurora Kinase Inhibitor VX-680 | Descriptor: | CYCLOPROPANECARBOXYLIC ACID {4-[4-(4-METHYL-PIPERAZIN-1-YL)-6-(5-METHYL-2H-PYRAZOL-3-YLAMINO)-PYRIMIDIN-2-YLSULFANYL]-PHENYL}-AMIDE, Proto-oncogene tyrosine-protein kinase ABL1 | Authors: | Young, M.A, Shah, N.P, Chao, L.H, Zarrinkar, P, Sawyers, P, Kuriyan, J. | Deposit date: | 2005-11-23 | Release date: | 2006-01-24 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (1.91 Å) | Cite: | Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680. Cancer Res., 66, 2006
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2FB8
| Structure of the B-Raf kinase domain bound to SB-590885 | Descriptor: | (1Z)-5-(2-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-PYRIDIN-4-YL-1H-IMIDAZOL-4-YL)INDAN-1-ONE OXIME, B-Raf proto-oncogene serine/threonine-protein kinase | Authors: | Lougheed, J.C, Lee, J, Chau, D.C, Stout, T.J. | Deposit date: | 2005-12-08 | Release date: | 2006-12-12 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res., 66, 2006
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2G2H
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2G15
| Structural Characterization of autoinhibited c-Met kinase | Descriptor: | activated met oncogene | Authors: | 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. | Deposit date: | 2006-02-13 | Release date: | 2006-03-21 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | 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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4UXQ
| FGFR4 in complex with Ponatinib | Descriptor: | 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 4, SULFATE ION | Authors: | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | Deposit date: | 2014-08-27 | Release date: | 2014-12-03 | Last modified: | 2014-12-17 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | 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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4UXL
| Structure of Human ROS1 Kinase Domain in Complex with PF-06463922 | Descriptor: | (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 | Authors: | McTigue, M, Deng, Y, Liu, W, Brooun, A, Stewart, A. | Deposit date: | 2014-08-25 | Release date: | 2015-03-11 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | 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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4UYA
| Structure of MLK4 kinase domain with ATPgammaS | Descriptor: | MAGNESIUM ION, MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE MLK4, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER | Authors: | Read, J.A, Brassington, C, Pollard, H.K, Phillips, C, Green, I, Overmann, R, Collier, M. | Deposit date: | 2014-08-29 | Release date: | 2015-09-30 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Recurrent Mlk4 Loss-of-Function Mutations Suppress Jnk Signaling to Promote Colon Tumorigenesis. Cancer Res., 76, 2016
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4WD5
| Crystal structure of EGFR 696-1022 T790M in complex with QL-X138 | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, N-{2-methyl-5-[2-oxo-9-(1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-1(2H)-yl]phenyl}propanamide | Authors: | Yun, C.H, Eck, M.J. | Deposit date: | 2014-09-07 | Release date: | 2016-05-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Crystal structure of EGFR 696-1022 T790M in complex with QL-X138 To Be Published
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4WA9
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4UWB
| Fibroblast growth factor receptor 1 kinase in complex with JK-P5 | Descriptor: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... | Authors: | Beeston, H, Tucker, J, Kankanala, J. | Deposit date: | 2014-08-11 | Release date: | 2015-09-02 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (2.31 Å) | Cite: | 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 | Descriptor: | 1,2-ETHANEDIOL, 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ... | Authors: | Beeston, H, Tucker, J, Kankanala, J. | Deposit date: | 2014-08-11 | Release date: | 2015-09-02 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (1.96 Å) | Cite: | 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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1OEC
| FGFr2 kinase domain | Descriptor: | 4-ARYL-2-PHENYLAMINO PYRIMIDINE, FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION | Authors: | Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J. | Deposit date: | 2003-03-24 | Release date: | 2004-10-27 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | The Crystal Structure of the Fgfr2 Tyrosine Kinase Domain in Complex with 4-Aryl-2-Phenylamino Pyrimidine Angiogenesis Inhibitors To be Published
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4UWY
| FGFR1 Apo structure | Descriptor: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | Authors: | Thiyagarajan, N, Bunney, T, Katan, M. | Deposit date: | 2014-08-15 | Release date: | 2015-02-25 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.305 Å) | Cite: | 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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1OPJ
| Structural basis for the auto-inhibition of c-Abl tyrosine kinase | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, MYRISTIC ACID, ... | Authors: | Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | Deposit date: | 2003-03-06 | Release date: | 2003-04-08 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Structural basis for the autoinhibition of c-Abl tyrosine kinase Cell(Cambridge,Mass.), 112, 2003
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4WKQ
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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 | Descriptor: | 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 | Authors: | Muckelbauer, J.K. | Deposit date: | 2014-10-16 | Release date: | 2015-03-18 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | 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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1P4O
| Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. | Descriptor: | Insulin-like growth factor I receptor protein | Authors: | Munshi, S, Kornienko, M, Hall, D.L, Darke, P.L, Waxman, L, Kuo, L.C. | Deposit date: | 2003-04-23 | Release date: | 2003-04-29 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution. Acta Crystallogr.,Sect.D, 59, 2003
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1P14
| Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase | Descriptor: | insulin receptor | Authors: | Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R. | Deposit date: | 2003-04-11 | Release date: | 2003-07-22 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor J.Biol.Chem., 278, 2003
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4WO5
| Crystal structure of a BRAF kinase domain monomer | Descriptor: | N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide, Serine/threonine-protein kinase B-raf | Authors: | Critton, D.A. | Deposit date: | 2014-10-15 | Release date: | 2014-12-03 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.83 Å) | Cite: | Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation. Nat.Struct.Mol.Biol., 22, 2015
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4WRG
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4X3J
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 1-[4-(4-amino-5-oxopyrido[2,3-d]pyrimidin-8(5H)-yl)phenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea, Angiopoietin-1 receptor | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-30 | Release date: | 2014-12-24 | Last modified: | 2015-01-21 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
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4WUN
| Structure of FGFR1 in complex with AZD4547 (N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE) at 1.65 angstrom | Descriptor: | 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 | Authors: | Squire, C.J, Yosaatmadja, C.J. | Deposit date: | 2014-11-02 | Release date: | 2014-11-19 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | The 1.65 angstrom resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition. Acta Crystallogr.,Sect.D, 71, 2015
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4WNM
| SYK catalytic domain in complex with a potent triazolopyridine inhibitor | Descriptor: | N~3~-(tetrahydro-2H-pyran-4-yl)-N~6~-[5-(tetrahydro-2H-pyran-4-ylmethyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]-1H-indazole-3,6-diamine, SULFATE ION, Tyrosine-protein kinase SYK | Authors: | Jackson, P.J. | Deposit date: | 2014-10-13 | Release date: | 2016-01-20 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation. Plos One, 11, 2016
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4XCU
| Crystal Structure of FGFR4 with an Irreversible Inhibitor | Descriptor: | Fibroblast growth factor receptor 4, N-(2-{[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino}-3-methylphenyl)propanamide, SULFATE ION | Authors: | Kim, J.L, Miduturu, C, Hodous, B, Brooijmans, N, Bifulco, N, Guzi, T. | Deposit date: | 2014-12-18 | Release date: | 2015-04-01 | Last modified: | 2018-12-12 | Method: | X-RAY DIFFRACTION (1.71 Å) | Cite: | First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov, 5, 2015
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