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2EB2
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Crystal structure of mutated EGFR kinase domain (G719S)
Descriptor: Epidermal growth factor receptor
Authors:Yoshikawa, S, Kukimoto-Niino, M, Chen, L, Liu, Z.J, Wang, B.C, Shirouzu, M, Senba, K, Yamamoto, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
Deposit date:2007-02-06
Release date:2008-02-12
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor
Oncogene, 2012
2B7A
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The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor
Descriptor: 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Tyrosine-protein kinase JAK2
Authors:Lucet, I.S, Fantino, E, Styles, M, Bamert, R, Patel, O, Broughton, S.E, Walter, M, Burns, C.J, Treutlein, H, Wilks, A.F, Rossjohn, J.
Deposit date:2005-10-04
Release date:2006-01-10
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2 Å)
Cite:The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.
Blood, 107, 2006
2EB3
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Crystal structure of mutated EGFR kinase domain (L858R) in complex with AMPPNP
Descriptor: Epidermal growth factor receptor, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER
Authors:Yoshikawa, S, Kukimoto-Niino, M, Shirouzu, M, Senba, K, Yamamoto, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
Deposit date:2007-02-06
Release date:2008-02-12
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (2.84 Å)
Cite:Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor
Oncogene, 2012
2ETM
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BU of 2etm by Molmil
Crystal Structure of Focal Adhesion Kinase Domain Complexed with 7H-Pyrrolo [2,3-d] pyrimidine Derivative
Descriptor: 7-PYRIDIN-2-YL-N-(3,4,5-TRIMETHOXYPHENYL)-7H-PYRROLO[2,3-D]PYRIMIDIN-2-AMINE, Focal adhesion kinase 1
Authors:Lee, C.C.
Deposit date:2005-10-27
Release date:2006-10-10
Last modified:2023-08-23
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Crystal Structure of Focal Adhesion Kinase Domain Complexed with ATP and novel 7H-Pyrrolo [2,3-d] pyrimidine scaffolds
To be Published
2FGI
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074
Descriptor: 1-TERT-BUTYL-3-[6-(3,5-DIMETHOXY-PHENYL)-2-(4-DIETHYLAMINO-BUTYLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-YL]-UREA, PROTEIN (FIBROBLAST GROWTH FACTOR (FGF) RECEPTOR 1)
Authors:Mohammadi, M, Froum, S, Hamby, J.M, Schroeder, M, Panek, R.L, Lu, G.H, Eliseenkova, A.V, Green, D, Schlessinger, J, Hubbard, S.R.
Deposit date:1998-09-15
Release date:1999-09-13
Last modified:2023-12-27
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain.
EMBO J., 17, 1998
2EVA
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Structural Basis for the Interaction of TAK1 Kinase with its Activating Protein TAB1
Descriptor: ADENOSINE, TAK1 kinase - TAB1 chimera fusion protein
Authors:Brown, K, Vial, S.C, Dedi, N, Long, J.M, Dunster, N.J, Cheetham, G.M.
Deposit date:2005-10-31
Release date:2006-05-02
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural basis for the interaction of TAK1 kinase with its activating protein TAB1
J.Mol.Biol., 354, 2005
1P4O
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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
1M17
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Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib
Descriptor: [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE, epidermal growth factor receptor
Authors:Stamos, J, Sliwkowski, M.X, Eigenbrot, C.
Deposit date:2002-06-17
Release date:2002-09-04
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor.
J.Biol.Chem., 277, 2002
1OEC
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BU of 1oec by Molmil
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
1M14
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Tyrosine Kinase Domain from Epidermal Growth Factor Receptor
Descriptor: Epidermal growth factor receptor
Authors:Stamos, J, Sliwkowski, M.X, Eigenbrot, C.
Deposit date:2002-06-17
Release date:2002-09-04
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor.
J.Biol.Chem., 277, 2002
1MP8
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Crystal structure of Focal Adhesion Kinase (FAK)
Descriptor: ADENOSINE-5'-DIPHOSPHATE, focal adhesion kinase 1
Authors:Nowakowski, J, Cronin, C.N, McRee, D.E, Knuth, M.W, Nelson, C.G, Pavletich, N.P, Rodgers, J, Sang, B.-C, Scheibe, D.N, Swanson, R.V, Thompson, D.A.
Deposit date:2002-09-11
Release date:2003-09-16
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography
Structure, 10, 2002
1M52
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Crystal Structure of the c-Abl Kinase domain in complex with PD173955
Descriptor: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 6-(2,6-DICHLORO-PHENYL)-8-METHYL-2-(3-METHYLSULFANYL-PHENYLAMINO)-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1
Authors:Nagar, B, Bornmann, W, Pellicena, P, Schindler, T, Veach, D, Miller, W.T, Clarkson, B, Kuriyan, J.
Deposit date:2002-07-08
Release date:2002-09-18
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Crystal Structures of the Kinase Domain of c-Abl in Complex with the Small Molecule Inhibitors PD173955 and Imatinib (STI-571)
Cancer Res., 62, 2002
1P14
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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
1PKG
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BU of 1pkg by Molmil
Structure of a c-Kit Kinase Product Complex
Descriptor: ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein
Authors:Mol, C.D, Lim, K.B, Sridhar, V, Zou, H, Chien, E.Y.T, Sang, B.-C, Nowakowski, J, Kassel, D.B, Cronin, C.N, McRee, D.E.
Deposit date:2003-06-05
Release date:2003-08-12
Last modified:2017-08-09
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation.
J.Biol.Chem., 278, 2003
1MQB
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Crystal Structure of Ephrin A2 (ephA2) Receptor Protein Kinase
Descriptor: Ephrin type-A receptor 2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER
Authors: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.
Deposit date:2002-09-16
Release date:2003-09-16
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Structures of the Cancer Related Aurora-A, FAK and EphA2 Protein Kinases from Nanovolume Crystallography
Structure, 10, 2003
1OPJ
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BU of 1opj by Molmil
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
1QPD
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STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS
Descriptor: LCK KINASE, STAUROSPORINE, SULFATE ION
Authors:Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A.
Deposit date:1999-05-24
Release date:2000-05-24
Last modified:2022-12-21
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
1QPE
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STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS
Descriptor: 1-TERT-BUTYL-3-(4-CHLORO-PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE, LCK KINASE, SULFATE ION
Authors:Zhu, X, Morgenstern, K.A.
Deposit date:1999-05-24
Release date:2000-05-31
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
1QPJ
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CRYSTAL STRUCTURE OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH STAUROSPORINE.
Descriptor: LCK TYROSINE KINASE, STAUROSPORINE, SULFATE ION
Authors:Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M.
Deposit date:1999-05-25
Release date:2000-05-31
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
4D2R
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Human IGF in complex with a Dyrk1B inhibitor
Descriptor: CHLORIDE ION, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR, N-{2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
Authors:Debreczeni, J.E, Kettle, J.G, Ballard, P, Bardelle, C, Butterworth, S, Colclough, N, Critchlow, S.E, Fairley, G, Fillery, S, Graham, M.A, Goodwin, L, Guichard, S, Hudson, K, Mahmood, A, Vincent, J, Ward, R.A, Whittaker, D.
Deposit date:2014-05-12
Release date:2015-04-22
Last modified:2024-05-08
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors to Explore a Mek Resistance Hypothesis.
J.Med.Chem., 58, 2015
4CLJ
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Structure of L1196M Mutant Human Anaplastic Lymphoma Kinase in Complex with PF-06463922 ((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).
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, ALK TYROSINE KINASE RECEPTOR
Authors:McTigue, M.A, Deng, Y.L, Liu, W, Brooun, A, Stewart, A.E.
Deposit date:2014-01-14
Release date:2014-05-28
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (1.66 Å)
Cite:Discovery of (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 (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations.
J.Med.Chem., 57, 2014
4CLI
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Structure of the Human Anaplastic Lymphoma Kinase in Complex with PF- 06463922 ((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).
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, ALK TYROSINE KINASE RECEPTOR
Authors:McTigue, M.A, Deng, Y.L, Liu, W, Brooun, A, Stewart, A.E.
Deposit date:2014-01-14
Release date:2014-05-28
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (2.05 Å)
Cite:Discovery of (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 (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations.
J.Med.Chem., 57, 2014
4CNH
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Structure of the Human Anaplastic Lymphoma Kinase in Complex with the inhibitor 3-((1R)-1-(5-fluoro-2-methoxyphenyl)ethoxy)-5-(1-methyl-1H- 1,2,3-triazol-5-yl)pyridin-2-amine
Descriptor: 3-[(1R)-1-(5-fluoro-2-methoxyphenyl)ethoxy]-5-(1-methyl-1H-1,2,3-triazol-5-yl)pyridin-2-amine, ALK TYROSINE KINASE RECEPTOR
Authors:McTigue, M.A, Deng, Y.L, Liu, W, Brooun, A, Stewart, A.E.
Deposit date:2014-01-22
Release date:2014-05-28
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Discovery of (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 (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations.
J.Med.Chem., 57, 2014
4CKI
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Crystal Structure of oncogenic RET tyrosine kinase M918T bound to adenosine
Descriptor: ADENOSINE, FORMIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET
Authors:Plaza-Menacho, I, Barnouin, K, Goodman, K, Martinez-Torres, R.J, Borg, A, Murray-Rust, J, Mouilleron, S, Knowles, P, McDonald, N.Q.
Deposit date:2014-01-06
Release date:2014-03-05
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (2.116 Å)
Cite:Oncogenic RET kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans.
Mol. Cell, 53, 2014
4CKJ
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Crystal structure of RET tyrosine kinase domain bound to adenosine
Descriptor: ADENOSINE, FORMIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET
Authors:Plaza-Menacho, I, Barnouin, K, Goodman, K, Martinez-Torres, R.J, Borg, A, Murray-Rust, J, Mouilleron, S, Knowles, P, McDonald, N.Q.
Deposit date:2014-01-06
Release date:2014-03-05
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (1.65 Å)
Cite:Oncogenic RET kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans.
Mol. Cell, 53, 2014

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