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1YWN
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Vegfr2 in complex with a novel 4-amino-furo[2,3-d]pyrimidine
分子名称: N-{4-[4-AMINO-6-(4-METHOXYPHENYL)FURO[2,3-D]PYRIMIDIN-5-YL]PHENYL}-N'-[2-FLUORO-5-(TRIFLUOROMETHYL)PHENYL]UREA, Vascular endothelial growth factor receptor 2
著者Miyazaki, Y, Matsunaga, S, Tang, J, Maeda, Y, Nakano, M, Philippe, R.J, Shibahara, M, Liu, W, Sato, H, Wang, L, Nolte, R.T.
登録日2005-02-18
公開日2005-08-23
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (1.71 Å)
主引用文献Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors
Bioorg.Med.Chem.Lett., 15, 2005
1YVJ
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Crystal structure of the Jak3 kinase domain in complex with a staurosporine analogue
分子名称: (2S,3S)-1,4-DIMERCAPTOBUTANE-2,3-DIOL, 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, Tyrosine-protein kinase JAK3
著者Boggon, T.J, Li, Y, Manley, P.W, Eck, M.J.
登録日2005-02-15
公開日2005-05-24
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog
Blood, 106, 2005
2B7A
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The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor
分子名称: 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Tyrosine-protein kinase JAK2
著者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.
登録日2005-10-04
公開日2006-01-10
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.
Blood, 107, 2006
2BDJ
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Src kinase in complex with inhibitor AP23464
分子名称: 3-[2-(2-CYCLOPENTYL-6-{[4-(DIMETHYLPHOSPHORYL)PHENYL]AMINO}-9H-PURIN-9-YL)ETHYL]PHENOL, Proto-oncogene tyrosine-protein kinase Src
著者Dalgarno, D, Stehle, T, Schelling, P, Narula, S, Sawyer, T.
登録日2005-10-20
公開日2006-10-24
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Chem.Biol.Drug Des., 67, 2006
2BDF
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Src kinase in complex with inhibitor AP23451
分子名称: Proto-oncogene tyrosine-protein kinase Src, {[(4-{[2-(4-AMINOCYCLOHEXYL)-9-ETHYL-9H-PURIN-6-YL]AMINO}PHENYL)(HYDROXY)PHOSPHORYL]METHYL}PHOSPHONIC ACID
著者Dalgarno, D, Stehle, T, Schelling, P, Sawyer, T, Narula, S.
登録日2005-10-20
公開日2006-10-24
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Chem.Biol.Drug Des., 67, 2006
2DQ7
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Crystal Structure of Fyn kinase domain complexed with staurosporine
分子名称: Proto-oncogene tyrosine-protein kinase Fyn, STAUROSPORINE
著者Kinoshita, T, Tada, T.
登録日2006-05-23
公開日2006-07-04
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献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
分子名称: 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
著者Horio, T, Hamasaki, T, Wakayama, T, Takagaki, K, Ohgi, T.
登録日2006-11-10
公開日2007-05-22
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献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)
分子名称: Epidermal growth factor receptor
著者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)
登録日2007-02-06
公開日2008-02-12
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献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
分子名称: Epidermal growth factor receptor, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER
著者Yoshikawa, S, Kukimoto-Niino, M, Shirouzu, M, Senba, K, Yamamoto, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-02-06
公開日2008-02-12
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.84 Å)
主引用文献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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Crystal Structure of Focal Adhesion Kinase Domain Complexed with 7H-Pyrrolo [2,3-d] pyrimidine Derivative
分子名称: 7-PYRIDIN-2-YL-N-(3,4,5-TRIMETHOXYPHENYL)-7H-PYRROLO[2,3-D]PYRIMIDIN-2-AMINE, Focal adhesion kinase 1
著者Lee, C.C.
登録日2005-10-27
公開日2006-10-10
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Crystal Structure of Focal Adhesion Kinase Domain Complexed with ATP and novel 7H-Pyrrolo [2,3-d] pyrimidine scaffolds
To be Published
1SM2
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Crystal structure of the phosphorylated Interleukin-2 tyrosine kinase catalytic domain
分子名称: STAUROSPORINE, Tyrosine-protein kinase ITK/TSK
著者Brown, K, Long, J.M, Vial, S.C.M, Dedi, N, Dunster, N.J, Renwick, S.B, Tanner, A.J, Frantz, J.D, Fleming, M.A, Cheetham, G.M.T.
登録日2004-03-08
公開日2004-07-16
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2.3 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
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
1T46
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STRUCTURAL BASIS FOR THE AUTOINHIBITION AND STI-571 INHIBITION OF C-KIT 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, Homo sapiens v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, PHOSPHATE ION
著者Mol, C.D, Dougan, D.R, Schneider, T.R, Skene, R.J, Kraus, M.L, Scheibe, D.N, Snell, G.P, Zou, H, Sang, B.C, Wilson, K.P.
登録日2004-04-28
公開日2004-06-15
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (1.6 Å)
主引用文献Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.
J.Biol.Chem., 279, 2004
1T45
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STRUCTURAL BASIS FOR THE AUTOINHIBITION AND STI-571 INHIBITION OF C-KIT TYROSINE KINASE
分子名称: Homo sapiens v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
著者Mol, C.D, Dougan, D.R, Schneider, T.R, Skene, R.J, Kraus, M.L, Scheibe, D.N, Snell, G.P, Zou, H, Sang, B.C, Wilson, K.P.
登録日2004-04-28
公開日2004-06-15
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.
J.Biol.Chem., 279, 2004
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
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
1UWJ
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The complex of mutant V599E B-RAF and BAY439006.
分子名称: 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE
著者Barford, D, Roe, S.M, Wan, P.T.C, Cancer Genome Project
登録日2004-02-05
公開日2004-03-19
最終更新日2018-01-17
実験手法X-RAY DIFFRACTION (3.5 Å)
主引用文献Mechanism of Activation of the Raf-Erk Signaling Pathway by Oncogenic Mutations of B-Raf
Cell(Cambridge,Mass.), 116, 2004
1UWH
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The complex of wild type B-RAF and BAY439006.
分子名称: 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE, CHLORIDE ION
著者Barford, D, Roe, S.M, Wan, P.T.C, Cancer Genome Project
登録日2004-02-05
公開日2004-03-19
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.95 Å)
主引用文献Mechanism of Activation of the Raf-Erk Signaling Pathway by Oncogenic Mutations of B-Raf
Cell(Cambridge,Mass.), 116, 2004
1VR2
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HUMAN VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 (KDR) KINASE DOMAIN
分子名称: PROTEIN (VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR KINASE)
著者Mctigue, M, Wickersham, J, Pinko, C, Showalter, R, Parast, C, Tempczyk-Russell, A, Gehring, M, Mroczkowski, B, Kan, C, Villafranca, J, Appelt, K.
登録日1998-12-03
公開日2000-03-15
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: a key enzyme in angiogenesis.
Structure Fold.Des., 7, 1999
1XBA
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Crystal structure of apo syk tyrosine kinase domain
分子名称: Tyrosine-protein kinase SYK
著者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, 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
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
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

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