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1BYG
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KINASE DOMAIN OF HUMAN C-TERMINAL SRC KINASE (CSK) IN COMPLEX WITH INHIBITOR STAUROSPORINE
分子名称: PROTEIN (C-TERMINAL SRC KINASE), STAUROSPORINE
著者Antson, A.A, Lamers, M.B.A.C, Scott, R.K, Williams, D.H, Hubbard, R.E.
登録日1998-10-14
公開日1999-10-14
最終更新日2023-08-09
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine.
J.Mol.Biol., 285, 1999
1AGW
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR
分子名称: 3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE, FGF RECEPTOR 1
著者Mohammadi, M, Schlessinger, J, Hubbard, S.R.
登録日1997-03-25
公開日1998-03-25
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.
Science, 276, 1997
1FGK
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1
分子名称: FGF RECEPTOR 1
著者Mohammadi, M, Schlessinger, J, Hubbard, S.R.
登録日1997-02-08
公開日1997-07-23
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism.
Cell(Cambridge,Mass.), 86, 1996
1FPU
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CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR
分子名称: N-[4-METHYL-3-[[4-(3-PYRIDINYL)-2-PYRIMIDINYL]AMINO]PHENYL]-3-PYRIDINECARBOXAMIDE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL
著者Schindler, T, Bornmann, W, Pellicena, P, Miller, W.T, Clarkson, B, Kuriyan, J.
登録日2000-08-31
公開日2000-09-20
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.
Science, 289, 2000
1FGI
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU5402 INHIBITOR
分子名称: 3-[(3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-YL)METHYLENE]-2-INDOLINONE, FGF RECEPTOR 1
著者Mohammadi, M, Schlessinger, J, Hubbard, S.R.
登録日1997-03-22
公開日1998-04-08
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.
Science, 276, 1997
1GAG
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CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR
分子名称: BISUBSTRATE PEPTIDE INHIBITOR, INSULIN RECEPTOR, TYROSINE KINASE DOMAIN, ...
著者Parang, K, Till, J.H, Ablooglu, A.J, Kohanski, R.A, Hubbard, S.R, Cole, P.A.
登録日2000-11-29
公開日2001-01-17
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Mechanism-based design of a protein kinase inhibitor.
Nat.Struct.Biol., 8, 2001
1FVR
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TIE2 KINASE DOMAIN
分子名称: TYROSINE-PROTEIN KINASE TIE-2
著者Shewchuk, L.M, Hassell, A.M, Ellis, B, Holmes, W.D, Davis, R, Horne, E.L, Kadwell, S.H, McKee, D.D, Moore, J.T.
登録日2000-09-20
公開日2001-09-20
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Structure of the Tie2 RTK domain: self-inhibition by the nucleotide binding loop, activation loop, and C-terminal tail.
Structure Fold.Des., 8, 2000
1GJO
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The FGFr2 tyrosine kinase domain
分子名称: FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION
著者Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J.
登録日2001-07-31
公開日2003-08-15
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献The Fgfr2 Tyrosine Kinase Domain
To be Published
8AAU
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LIM Domain Kinase 1 (LIMK1) bound to LIMKi3
分子名称: 1,2-ETHANEDIOL, LIM domain kinase 1, MAGNESIUM ION, ...
著者Mathea, S, Salah, E, Hanke, T, Knapp, S.
登録日2022-07-03
公開日2022-08-10
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (1.74 Å)
主引用文献Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
J.Med.Chem., 65, 2022
7ZVS
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Crystal structure of the Schistosoma mansoni VKR2 kinase domain in an active-like state (ADP-bound)
分子名称: ADENOSINE-5'-DIPHOSPHATE, Venus kinase receptor 2
著者Beis, K, Mathavan, I.
登録日2022-05-17
公開日2022-10-12
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (3.07 Å)
主引用文献Identification of Inhibitors of the Schistosoma mansoni VKR2 Kinase Domain.
Acs Med.Chem.Lett., 13, 2022
8A27
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EGFR kinase domain in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide
分子名称: (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, 1,2-ETHANEDIOL, Epidermal growth factor receptor, ...
著者Kuglstatter, A, Ehler, A.
登録日2022-06-02
公開日2022-10-19
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.07 Å)
主引用文献Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
J.Med.Chem., 65, 2022
8A2A
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EGFR kinase domain in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide (form 2)
分子名称: (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, Epidermal growth factor receptor, SULFATE ION
著者Kuglstatter, A, Ehler, A.
登録日2022-06-03
公開日2022-10-19
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.43 Å)
主引用文献Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
J.Med.Chem., 65, 2022
8A2D
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EGFR kinase domain (L858R/V948R) in complex with 2-[4-(difluoromethyl)-6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-7-methyl-indazol-2-yl]-2-spiro[6,7-dihydropyrrolo[1,2-c]imidazole-5,1'-cyclopropane]-1-yl-N-thiazol-2-yl-acetamide
分子名称: (2R)-2-[4-[bis(fluoranyl)methyl]-6-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-7-methyl-indazol-2-yl]-2-spiro[6,7-dihydropyrrolo[1,2-c]imidazole-5,1'-cyclopropane]-1-yl-N-(1,3-thiazol-2-yl)ethanamide, 1,2-ETHANEDIOL, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ...
著者Kuglstatter, A, Ehler, A.
登録日2022-06-03
公開日2022-10-19
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.11 Å)
主引用文献Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
J.Med.Chem., 65, 2022
8A2B
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EGFR kinase domain (L858R/V948R) in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide
分子名称: (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, Epidermal growth factor receptor
著者Kuglstatter, A, Ehler, A.
登録日2022-06-03
公開日2022-10-19
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.69 Å)
主引用文献Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
J.Med.Chem., 65, 2022
4V01
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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}benzamide, 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2018-04-04
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
4UXQ
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FGFR4 in complex with Ponatinib
分子名称: 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
著者Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A.
登録日2014-08-27
公開日2014-12-03
最終更新日2014-12-17
実験手法X-RAY DIFFRACTION (1.85 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
4V0G
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JAK3 in complex with a covalent EGFR inhibitor
分子名称: N-[3-(2-{3-amino-6-[1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]pyrazin-2-yl}-1H-benzimidazol-1-yl)phenyl]propanamide, TYROSINE-PROTEIN KINASE JAK3
著者Debreczeni, J.E, Hennessy, E.J, Chuaquini, C, Ashton, S, Coclough, N, Cross, D.A.E, Eberlein, C, Gingipalli, L, Klinowska, T.C.M, Orme, J.P, Sha, L, Wu, X.
登録日2014-09-16
公開日2016-01-13
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献Utilisation of Structure Based Design to Identify Novel, Irreversible Inhibitors of the Epidermal Growth Factor Receptor (Egfr) Harboring the Gatekeeper T790M Mutation
To be Published
4UWY
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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
4WD5
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Crystal structure of EGFR 696-1022 T790M in complex with QL-X138
分子名称: 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
著者Yun, C.H, Eck, M.J.
登録日2014-09-07
公開日2016-05-04
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (3.3 Å)
主引用文献Crystal structure of EGFR 696-1022 T790M in complex with QL-X138
To Be Published
4WA9
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The crystal structure of human abl1 wild type kinase domain in complex with axitinib
分子名称: AXITINIB, Tyrosine-protein kinase ABL1
著者Johnson, E, McTigue, M, Cronin, C.N.
登録日2014-08-28
公開日2015-02-11
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.
Nature, 519, 2015
4UWB
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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2021-06-16
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
4UWC
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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2021-06-16
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
4UXL
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Structure of Human ROS1 Kinase Domain in Complex with PF-06463922
分子名称: (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
著者McTigue, M, Deng, Y, Liu, W, Brooun, A, Stewart, A.
登録日2014-08-25
公開日2015-03-11
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献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
4UYA
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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
4WKQ
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1.85 angstrom structure of EGFR kinase domain with gefitinib
分子名称: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Epidermal growth factor receptor, Gefitinib, ...
著者Yosaatmadja, Y, Squire, C.J.
登録日2014-10-03
公開日2014-11-05
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献1.85 angstrom structure of EGFR kinase domain with gefitinib
To Be Published

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件を2024-03-27に公開中

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