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2DQ7
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Crystal Structure of Fyn kinase domain complexed with staurosporine
Descriptor: Proto-oncogene tyrosine-protein kinase Fyn, STAUROSPORINE
Authors:Kinoshita, T, Tada, T.
Deposit date:2006-05-23
Release date:2006-07-04
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Structure of human Fyn kinase domain complexed with staurosporine.
Biochem.Biophys.Res.Commun., 346, 2006
2E2B
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Crystal structure of the c-Abl kinase domain in complex with INNO-406
Descriptor: N-[3-(4,5'-BIPYRIMIDIN-2-YLAMINO)-4-METHYLPHENYL]-4-{[(3S)-3-(DIMETHYLAMINO)PYRROLIDIN-1-YL]METHYL}-3-(TRIFLUOROMETHYL) BENZAMIDE, Proto-oncogene tyrosine-protein kinase ABL1
Authors:Horio, T, Hamasaki, T, Wakayama, T, Takagaki, K, Ohgi, T.
Deposit date:2006-11-10
Release date:2007-05-22
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives
Bioorg.Med.Chem.Lett., 17, 2007
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
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
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
2ETM
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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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BU of 2fgi by Molmil
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
2F4J
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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
2FB8
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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
2G2H
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A Src-like Inactive Conformation in the Abl Tyrosine Kinase Domain
Descriptor: 6-(2,6-DICHLOROPHENYL)-2-{[3-(HYDROXYMETHYL)PHENYL]AMINO}-8-METHYLPYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, Abl Tyrosine
Authors:Levinson, N.M, Kuchment, O.
Deposit date:2006-02-16
Release date:2006-05-23
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2 Å)
Cite:A SRC-like inactive conformation in the abl tyrosine kinase domain.
Plos Biol., 4, 2006
2G2F
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A Src-like Inactive Conformation in the Abl Tyrosine Kinase Domain
Descriptor: ATP-Peptide Conjugate, Abl Kinase, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, ...
Authors:Levinson, N.M, Kuchment, O.
Deposit date:2006-02-15
Release date:2006-05-23
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:A SRC-like inactive conformation in the abl tyrosine kinase domain.
Plos Biol., 4, 2006
2G15
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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
2G2I
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A Src-like Inactive Conformation in the Abl Tyrosine Kinase Domain
Descriptor: ADENOSINE-5'-DIPHOSPHATE, ATP-Peptide Conjugate, Abl Tyrosine Kinase
Authors:Levinson, N.M, Kuchment, O.
Deposit date:2006-02-16
Release date:2006-05-23
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (3.12 Å)
Cite:A SRC-like inactive conformation in the abl tyrosine kinase domain.
Plos Biol., 4, 2006
2G1T
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A Src-like Inactive Conformation in the Abl Tyrosine Kinase Domain
Descriptor: ATP-Peptide Conjugate, MAGNESIUM ION, Proto-oncogene tyrosine-protein kinase ABL1, ...
Authors:Levinson, N.M, Kuchment, O.
Deposit date:2006-02-14
Release date:2006-05-23
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:A SRC-like inactive conformation in the abl tyrosine kinase domain.
Plos Biol., 4, 2006
2GS6
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Crystal Structure of the active EGFR kinase domain in complex with an ATP analog-peptide conjugate
Descriptor: CHLORIDE ION, Epidermal growth factor receptor, Peptide, ...
Authors:Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J.
Deposit date:2006-04-25
Release date:2006-06-20
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:An Allosteric Mechanism for Activation of the Kinase Domain of Epidermal Growth Factor Receptor
Cell(Cambridge,Mass.), 125, 2006
2GQG
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BU of 2gqg by Molmil
X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain
Descriptor: GLYCEROL, N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, Proto-oncogene tyrosine-protein kinase ABL1
Authors:Klei, H.E.
Deposit date:2006-04-20
Release date:2006-11-21
Last modified:2017-10-18
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:The Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain Elucidates Its Inhibitory Activity against Imatinib-Resistant ABL Mutants
CANCER RES., 66, 2006
2HEN
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BU of 2hen by Molmil
Crystal Structure of the EphB2 Receptor Kinase domain in complex with ADP
Descriptor: ADENOSINE-5'-DIPHOSPHATE, Ephrin type-B receptor 2, MAGNESIUM ION
Authors:Wybenga-Groot, L.E, Sicheri, F, Pawson, T.
Deposit date:2006-06-21
Release date:2007-02-13
Last modified:2024-02-14
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:A change in conformational dynamics underlies the activation of Eph receptor tyrosine kinases
EMBO J., 25, 2006
2GS7
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Crystal Structure of the inactive EGFR kinase domain in complex with AMP-PNP
Descriptor: Epidermal growth factor receptor, IODIDE ION, MAGNESIUM ION, ...
Authors:Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J.
Deposit date:2006-04-25
Release date:2006-06-20
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
Cell(Cambridge,Mass.), 125, 2006
2GS2
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Crystal Structure of the active EGFR kinase domain
Descriptor: Epidermal growth factor receptor
Authors:Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J.
Deposit date:2006-04-25
Release date:2006-06-20
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor.
Cell(Cambridge,Mass.), 125, 2006
2HIW
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BU of 2hiw by Molmil
Crystal Structure of Inactive Conformation Abl Kinase Catalytic Domain Complexed with Type II Inhibitor
Descriptor: 7-AMINO-1-METHYL-3-(2-METHYL-5-{[3-(TRIFLUOROMETHYL)BENZOYL]AMINO}PHENYL)-2-OXO-2,3-DIHYDROPYRIMIDO[4,5-D]PYRIMIDIN-1-IUM, Proto-oncogene tyrosine-protein kinase ABL1
Authors:Lee, C.
Deposit date:2006-06-29
Release date:2006-08-22
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:A general strategy for creating
Chem.Biol., 13, 2006
7REE
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BU of 7ree by Molmil
High-resolution crystal structure of human JAK2 kinase domain (JH1) bound to YM2-059
Descriptor: Tyrosine-protein kinase JAK2, [3-(4-{2-[3,5-difluoro-4-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}-1H-pyrazol-1-yl)-1-(ethanesulfonyl)azetidin-3-yl]acetonitrile
Authors:Karim, M.R, Schonbrunn, E.
Deposit date:2021-07-12
Release date:2021-09-01
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (1.38 Å)
Cite:High-resolution crystal structure of human JAK2 kinase domain (JH1) bound to YM2-059.
To Be Published
7R60
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BTK in complex with 18A
Descriptor: 2-(4-phenoxyphenoxy)-5-[(3R)-1-(prop-2-enoyl)piperidin-3-yl]pyridine-3-carboxamide, Tyrosine-protein kinase BTK
Authors:Gardberg, A.
Deposit date:2021-06-22
Release date:2021-10-06
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.94 Å)
Cite:Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity.
Chemmedchem, 16, 2021
7R61
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BTK in complex with 25A
Descriptor: 5-{(3S)-1-[(Z)-iminomethyl]piperidin-3-yl}-2-(4-phenoxyphenoxy)pyridine-3-carboxamide, DIMETHYL SULFOXIDE, Tyrosine-protein kinase BTK
Authors:Gardberg, A.
Deposit date:2021-06-22
Release date:2021-10-06
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.52 Å)
Cite:Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity.
Chemmedchem, 16, 2021
7RN6
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High-resolution crystal structure of human JAK2 kinase domain (JH1) bound to type-II inhibitor BBT594
Descriptor: 1,2-ETHANEDIOL, 5-{[6-(acetylamino)pyrimidin-4-yl]oxy}-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-2,3-dihydro-1H-indole-1-carboxamide, Tyrosine-protein kinase JAK2
Authors:Karim, M.R, Schonbrunn, E.
Deposit date:2021-07-29
Release date:2021-11-03
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (1.5 Å)
Cite:High-resolution crystal structure of human JAK2 kinase domain (JH1) bound to type-II inhibitor BBT594
To Be Published
7RUN
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Crystal structure of phosphorylated RET tyrosine kinase domain complexed with a pyrrolo[2,3-d]pyrimidine inhibitor.
Descriptor: 1-(4-{(1s,3s)-3-[4-amino-5-(3-amino-4-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl}piperazin-1-yl)ethan-1-one, CHLORIDE ION, Proto-oncogene tyrosine-protein kinase receptor Ret
Authors:Lee, C.C, Spraggon, G.
Deposit date:2021-08-17
Release date:2022-01-19
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (3.51 Å)
Cite:Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3- d ]pyrimidine RET Inhibitors.
Acs Med.Chem.Lett., 12, 2021

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