1YWN
 
 | | Vegfr2 in complex with a novel 4-amino-furo[2,3-d]pyrimidine | | Descriptor: | 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 | | Authors: | Miyazaki, Y, Matsunaga, S, Tang, J, Maeda, Y, Nakano, M, Philippe, R.J, Shibahara, M, Liu, W, Sato, H, Wang, L, Nolte, R.T. | | Deposit date: | 2005-02-18 | | Release date: | 2005-08-23 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.71 Å) | | Cite: | Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors
Bioorg.Med.Chem.Lett., 15, 2005
|
|
1YVJ
 | | Crystal structure of the Jak3 kinase domain in complex with a staurosporine analogue | | Descriptor: | (2S,3S)-1,4-DIMERCAPTOBUTANE-2,3-DIOL, 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, Tyrosine-protein kinase JAK3 | | Authors: | Boggon, T.J, Li, Y, Manley, P.W, Eck, M.J. | | Deposit date: | 2005-02-15 | | Release date: | 2005-05-24 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog
Blood, 106, 2005
|
|
2B7A
 | | 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
|
|
2BDJ
 | | Src kinase in complex with inhibitor AP23464 | | Descriptor: | 3-[2-(2-CYCLOPENTYL-6-{[4-(DIMETHYLPHOSPHORYL)PHENYL]AMINO}-9H-PURIN-9-YL)ETHYL]PHENOL, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Dalgarno, D, Stehle, T, Schelling, P, Narula, S, Sawyer, T. | | Deposit date: | 2005-10-20 | | Release date: | 2006-10-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | 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
 | | Src kinase in complex with inhibitor AP23451 | | Descriptor: | Proto-oncogene tyrosine-protein kinase Src, {[(4-{[2-(4-AMINOCYCLOHEXYL)-9-ETHYL-9H-PURIN-6-YL]AMINO}PHENYL)(HYDROXY)PHOSPHORYL]METHYL}PHOSPHONIC ACID | | Authors: | Dalgarno, D, Stehle, T, Schelling, P, Sawyer, T, Narula, S. | | Deposit date: | 2005-10-20 | | Release date: | 2006-10-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | 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
 | |
2E2B
 | | 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
 | | 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
 | | 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
 | |
1SM2
 | | Crystal structure of the phosphorylated Interleukin-2 tyrosine kinase catalytic domain | | Descriptor: | STAUROSPORINE, Tyrosine-protein kinase ITK/TSK | | Authors: | 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. | | Deposit date: | 2004-03-08 | | Release date: | 2004-07-16 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.
J.Biol.Chem., 279, 2004
|
|
1SNX
 | | CRYSTAL STRUCTURE OF APO INTERLEUKIN-2 TYROSINE KINASE CATALYTIC DOMAIN | | Descriptor: | Tyrosine-protein kinase ITK/TSK | | Authors: | 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. | | Deposit date: | 2004-03-12 | | Release date: | 2004-07-20 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.
J.Biol.Chem., 279, 2004
|
|
1T46
 | | STRUCTURAL BASIS FOR THE AUTOINHIBITION AND STI-571 INHIBITION OF C-KIT TYROSINE KINASE | | Descriptor: | 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 | | Authors: | 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. | | Deposit date: | 2004-04-28 | | Release date: | 2004-06-15 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.
J.Biol.Chem., 279, 2004
|
|
1T45
 | | STRUCTURAL BASIS FOR THE AUTOINHIBITION AND STI-571 INHIBITION OF C-KIT TYROSINE KINASE | | Descriptor: | Homo sapiens v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog | | Authors: | 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. | | Deposit date: | 2004-04-28 | | Release date: | 2004-06-15 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.
J.Biol.Chem., 279, 2004
|
|
1U4D
 | | Structure of the ACK1 Kinase Domain bound to Debromohymenialdisine | | Descriptor: | Activated CDC42 kinase 1, CHLORIDE ION, DEBROMOHYMENIALDISINE | | Authors: | Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J. | | Deposit date: | 2004-07-23 | | Release date: | 2004-08-31 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
|
|
1U46
 | | Crystal Structure of the Unphosphorylated Kinase Domain of the Tyrosine Kinase ACK1 | | Descriptor: | Activated CDC42 kinase 1, CHLORIDE ION | | Authors: | Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J. | | Deposit date: | 2004-07-23 | | Release date: | 2004-08-31 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
|
|
1U59
 | | Crystal Structure of the ZAP-70 Kinase Domain in Complex with Staurosporine | | Descriptor: | STAUROSPORINE, Tyrosine-protein kinase ZAP-70 | | Authors: | 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. | | Deposit date: | 2004-07-27 | | Release date: | 2004-08-17 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | 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
 | | Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the CDC42-associated Tyrosine Kinase ACK1 bound to AMP-PCP | | Descriptor: | Activated CDC42 kinase 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER | | Authors: | Lougheed, J.C, Chen, R.H, Mak, P, Stout, T.J. | | Deposit date: | 2004-07-26 | | Release date: | 2004-08-31 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal Structures of the Phosphorylated and Unphosphorylated Kinase Domains of the Cdc42-associated Tyrosine Kinase ACK1.
J.Biol.Chem., 279, 2004
|
|
1UWJ
 | | The complex of mutant V599E B-RAF and BAY439006. | | Descriptor: | 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE | | Authors: | Barford, D, Roe, S.M, Wan, P.T.C, Cancer Genome Project | | Deposit date: | 2004-02-05 | | Release date: | 2004-03-19 | | Last modified: | 2018-01-17 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Mechanism of Activation of the Raf-Erk Signaling Pathway by Oncogenic Mutations of B-Raf
Cell(Cambridge,Mass.), 116, 2004
|
|
1UWH
 | | The complex of wild type B-RAF and BAY439006. | | Descriptor: | 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 | | Authors: | Barford, D, Roe, S.M, Wan, P.T.C, Cancer Genome Project | | Deposit date: | 2004-02-05 | | Release date: | 2004-03-19 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Mechanism of Activation of the Raf-Erk Signaling Pathway by Oncogenic Mutations of B-Raf
Cell(Cambridge,Mass.), 116, 2004
|
|
1VR2
 | | HUMAN VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 (KDR) KINASE DOMAIN | | Descriptor: | PROTEIN (VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR KINASE) | | Authors: | Mctigue, M, Wickersham, J, Pinko, C, Showalter, R, Parast, C, Tempczyk-Russell, A, Gehring, M, Mroczkowski, B, Kan, C, Villafranca, J, Appelt, K. | | Deposit date: | 1998-12-03 | | Release date: | 2000-03-15 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | 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
 | | Crystal structure of apo syk tyrosine kinase domain | | Descriptor: | Tyrosine-protein kinase SYK | | Authors: | 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. | | Deposit date: | 2004-08-30 | | Release date: | 2004-11-02 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase.
J.Biol.Chem., 279, 2004
|
|
1XBB
 | | Crystal structure of the syk tyrosine kinase domain with Gleevec | | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Tyrosine-protein kinase SYK | | Authors: | 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. | | Deposit date: | 2004-08-30 | | Release date: | 2004-11-02 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.57 Å) | | Cite: | A Novel Mode of Gleevec Binding Is Revealed by the Structure of Spleen Tyrosine Kinase
J.Biol.Chem., 279, 2004
|
|
1XBC
 | | Crystal structure of the syk tyrosine kinase domain with Staurosporin | | Descriptor: | STAUROSPORINE, Tyrosine-protein kinase SYK | | Authors: | 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. | | Deposit date: | 2004-08-30 | | Release date: | 2004-11-02 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase
J.Biol.Chem., 279, 2004
|
|
1XKK
 | | EGFR kinase domain complexed with a quinazoline inhibitor- GW572016 | | Descriptor: | 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 | | Authors: | 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. | | Deposit date: | 2004-09-29 | | Release date: | 2004-12-07 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | 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
|
|
