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1YOM
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Crystal structure of Src kinase domain in complex with Purvalanol A
分子名称: 2-({6-[(3-CHLOROPHENYL)AMINO]-9-ISOPROPYL-9H-PURIN-2-YL}AMINO)-3-METHYLBUTAN-1-OL, Proto-oncogene tyrosine-protein kinase Src
著者Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A.
登録日2005-01-27
公開日2006-01-27
最終更新日2024-05-29
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Crystal structures of active SRC kinase domain complexes
J.Mol.Biol., 353, 2005
1XBB
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Crystal structure of the syk tyrosine kinase domain with Gleevec
分子名称: 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Tyrosine-protein kinase SYK
著者Nienaber, V.L, Atwell, S, Adams, J.M, Badger, J, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G.
登録日2004-08-30
公開日2004-11-02
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (1.57 Å)
主引用文献A Novel Mode of Gleevec Binding Is Revealed by the Structure of Spleen Tyrosine Kinase
J.Biol.Chem., 279, 2004
1XBC
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Crystal structure of the syk tyrosine kinase domain with Staurosporin
分子名称: STAUROSPORINE, Tyrosine-protein kinase SYK
著者Badger, J, Atwell, S, Adams, J.M, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Nienaber, V.L, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G.
登録日2004-08-30
公開日2004-11-02
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase
J.Biol.Chem., 279, 2004
1YI6
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C-term tail segment of human tyrosine kinase (258-533)
分子名称: Proto-oncogene tyrosine-protein kinase Src
著者Fleury, D, Sarubbi, E, Courjaud, A, Guitton, J.D, Ducruix, A.
登録日2005-01-11
公開日2006-05-02
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structure of the unphosphorylated C-terminal tail segment of the SRC kinase and its role in SRC activity regulation
To be published
1Y6A
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Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor
分子名称: N-[5-(ETHYLSULFONYL)-2-METHOXYPHENYL]-5-[3-(2-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-AMINE, Vascular endothelial growth factor receptor 2
著者Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A.
登録日2004-12-05
公開日2005-06-07
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J.Med.Chem., 48, 2005
1Y6B
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Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor
分子名称: N-(CYCLOPROPYLMETHYL)-4-(METHYLOXY)-3-({5-[3-(3-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-YL}AMINO)BENZENESULFONAMIDE, Vascular endothelial growth factor receptor 2
著者Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A.
登録日2004-12-05
公開日2005-06-07
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J.Med.Chem., 48, 2005
1XKK
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EGFR kinase domain complexed with a quinazoline inhibitor- GW572016
分子名称: Epidermal growth factor receptor, N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE, PHOSPHATE ION
著者Wood, E.R, Truesdale, A.T, McDonald, O.B, Yuan, D, Hassell, A, Dickerson, S.H, Ellis, B, Pennisi, C, Horne, E, Lackey, K, Alligood, K.J, Rusnak, D.W, Gilmer, T.M, Shewchuk, L.M.
登録日2004-09-29
公開日2004-12-07
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells.
Cancer Res., 64, 2004
8YGX
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Structure of the PYK2 from Biortus.
分子名称: Protein-tyrosine kinase 2-beta
著者Wang, F, Cheng, W, Lv, Z, Meng, Q, Zhang, B.
登録日2024-02-27
公開日2024-03-13
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structure of the PYK2 from Biortus.
To Be Published
8W3W
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Crystal structure of IRAK4 in complex with compound 4
分子名称: 7-methoxy-1-{[(2S)-5-oxopyrrolidin-2-yl]methoxy}isoquinoline-6-carboxamide, Interleukin-1 receptor-associated kinase 4
著者Han, S, Knafels, J.D.
登録日2024-02-22
公開日2024-05-01
実験手法X-RAY DIFFRACTION (1.976 Å)
主引用文献In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Acs Med.Chem.Lett., 15, 2024
8YGZ
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The Crystal Structure of TGF beta R2 kinase domain from Biortus.
分子名称: 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, TGF-beta receptor type-2
著者Wang, F, Cheng, W, Lv, Z, Ju, C, Wang, J.
登録日2024-02-27
公開日2024-03-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献The Crystal Structure of TGF beta R2 kinase domain from Biortus.
To Be Published
1SNX
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CRYSTAL STRUCTURE OF APO INTERLEUKIN-2 TYROSINE KINASE CATALYTIC DOMAIN
分子名称: Tyrosine-protein kinase ITK/TSK
著者Brown, K, Long, J.M, Vial, S.C, Dedi, N, Dunster, N.J, Renwick, S.B, Tanner, A.J, Frantz, J.D, Fleming, M.A, Cheetham, G.M.T.
登録日2004-03-12
公開日2004-07-20
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (3.2 Å)
主引用文献Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.
J.Biol.Chem., 279, 2004
8XLO
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FGFR1 kinase domain with a dual-warhead covalent inhibitor CXF-007
分子名称: CXF007, Fibroblast growth factor receptor 1, SULFATE ION
著者Chen, X.J, Chen, Y.H.
登録日2023-12-26
公開日2024-03-27
実験手法X-RAY DIFFRACTION (2.36 Å)
主引用文献Design, synthesis, and biological evaluation of selective covalent inhibitors of FGFR4.
Eur.J.Med.Chem., 268, 2024
8XLQ
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FGFR4 kinase domain with a dual-warhead covalent inhibitor CXF-007
分子名称: CXF007, Fibroblast growth factor receptor 4, SULFATE ION
著者Chen, X.J, Chen, Y.H.
登録日2023-12-26
公開日2024-03-27
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Design, synthesis, and biological evaluation of selective covalent inhibitors of FGFR4.
Eur.J.Med.Chem., 268, 2024
8XPV
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The Crystal Structure of EphA2 from Biortus.
分子名称: 1,2-ETHANEDIOL, 1-(3,3-dimethylbutyl)-3-{2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl}urea, Ephrin type-A receptor 2, ...
著者Wang, F, Cheng, W, Lv, Z, Meng, Q, Xu, Y.
登録日2024-01-04
公開日2024-01-24
実験手法X-RAY DIFFRACTION (1.55 Å)
主引用文献The Crystal Structure of EphA2 from Biortus.
To Be Published
8W3X
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Crystal structure of IRAK4 in complex with compound 6
分子名称: 7-ethoxy-1-{[(2S)-5-oxopyrrolidin-2-yl]methoxy}isoquinoline-6-carboxamide, Interleukin-1 receptor-associated kinase 4
著者Han, S, Knafels, J.D.
登録日2024-02-22
公開日2024-05-01
実験手法X-RAY DIFFRACTION (1.765 Å)
主引用文献In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Acs Med.Chem.Lett., 15, 2024
8XOX
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The Crystal Structure of FAK2 from Biortus.
分子名称: 1,2-ETHANEDIOL, N-methyl-N-{3-[({2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl}amino)methyl]pyridin-2-yl}methanesulfonamide, Protein-tyrosine kinase 2-beta
著者Wang, F, Cheng, W, Lv, Z, Ju, C, Wang, J.
登録日2024-01-02
公開日2024-01-24
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献The Crystal Structure of FAK2 from Biortus.
To Be Published
8W1L
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Structure of CSF1R kinase domain in complex with Cpd 32
分子名称: GLYCEROL, Macrophage colony-stimulating factor 1 receptor,CSF1R, SULFATE ION, ...
著者Kothe, M, Chodaparambil, J.
登録日2024-02-16
公開日2024-05-29
実験手法X-RAY DIFFRACTION (2.26 Å)
主引用文献Identification of Selective Imidazopyridine CSF1R Inhibitors.
Acs Med.Chem.Lett., 15, 2024
1P14
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Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase
分子名称: insulin receptor
著者Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R.
登録日2003-04-11
公開日2003-07-22
最終更新日2023-08-16
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor
J.Biol.Chem., 278, 2003
1U4D
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Structure of the ACK1 Kinase Domain bound to Debromohymenialdisine
分子名称: Activated CDC42 kinase 1, CHLORIDE ION, DEBROMOHYMENIALDISINE
著者Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J.
登録日2004-07-23
公開日2004-08-31
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
1U46
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Crystal Structure of the Unphosphorylated Kinase Domain of the Tyrosine Kinase ACK1
分子名称: Activated CDC42 kinase 1, CHLORIDE ION
著者Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J.
登録日2004-07-23
公開日2004-08-31
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
1U59
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Crystal Structure of the ZAP-70 Kinase Domain in Complex with Staurosporine
分子名称: STAUROSPORINE, Tyrosine-protein kinase ZAP-70
著者Jin, L, Pluskey, S, Petrella, E.C, Cantin, S.M, Gorga, J.C, Rynkiewicz, M.J, Pandey, P, Strickler, J.E, Babine, R.E, Weaver, D.T, Seidl, K.J.
登録日2004-07-27
公開日2004-08-17
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The Three-dimensional Structure of the ZAP-70 Kinase Domain in Complex with Staurosporine: IMPLICATIONS FOR THE DESIGN OF SELECTIVE INHIBITORS
J.Biol.Chem., 279, 2004
1PKG
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Structure of a c-Kit Kinase Product Complex
分子名称: ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein
著者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.
登録日2003-06-05
公開日2003-08-12
最終更新日2017-08-09
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation.
J.Biol.Chem., 278, 2003
1U54
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Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the CDC42-associated Tyrosine Kinase ACK1 bound to AMP-PCP
分子名称: Activated CDC42 kinase 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER
著者Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J.
登録日2004-07-26
公開日2004-08-31
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
1OPJ
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Structural basis for the auto-inhibition of c-Abl tyrosine kinase
分子名称: 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, MYRISTIC ACID, ...
著者Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J.
登録日2003-03-06
公開日2003-04-08
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (1.75 Å)
主引用文献Structural basis for the autoinhibition of c-Abl tyrosine kinase
Cell(Cambridge,Mass.), 112, 2003
1RJB
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Crystal Structure of FLT3
分子名称: FL cytokine receptor
著者Griffith, J, Black, J, Faerman, C, Swenson, L, Wynn, M, Lu, F, Lippke, J, Saxena, K.
登録日2003-11-19
公開日2004-02-03
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献The structural basis for autoinhibition of FLT3 by the juxtamembrane domain.
Mol.Cell, 13, 2004

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