2F4J
 
 | | 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
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2FB8
 | | 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
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2G2H
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2G15
 | | 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
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2G2F
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1OEC
 | | FGFr2 kinase domain | | Descriptor: | 4-ARYL-2-PHENYLAMINO PYRIMIDINE, FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION | | Authors: | Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J. | | Deposit date: | 2003-03-24 | | Release date: | 2004-10-27 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | The Crystal Structure of the Fgfr2 Tyrosine Kinase Domain in Complex with 4-Aryl-2-Phenylamino Pyrimidine Angiogenesis Inhibitors
To be Published
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1OPJ
 | | Structural basis for the auto-inhibition of c-Abl tyrosine kinase | | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, MYRISTIC ACID, ... | | Authors: | Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | | Deposit date: | 2003-03-06 | | Release date: | 2003-04-08 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Structural basis for the autoinhibition of c-Abl tyrosine kinase
Cell(Cambridge,Mass.), 112, 2003
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1P4O
 | | Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. | | Descriptor: | Insulin-like growth factor I receptor protein | | Authors: | Munshi, S, Kornienko, M, Hall, D.L, Darke, P.L, Waxman, L, Kuo, L.C. | | Deposit date: | 2003-04-23 | | Release date: | 2003-04-29 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution.
Acta Crystallogr.,Sect.D, 59, 2003
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1P14
 | | Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase | | Descriptor: | insulin receptor | | Authors: | Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R. | | Deposit date: | 2003-04-11 | | Release date: | 2003-07-22 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor
J.Biol.Chem., 278, 2003
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1PKG
 | | Structure of a c-Kit Kinase Product Complex | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein | | Authors: | 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. | | Deposit date: | 2003-06-05 | | Release date: | 2003-08-12 | | Last modified: | 2017-08-09 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation.
J.Biol.Chem., 278, 2003
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1QPD
 | | STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS | | Descriptor: | LCK KINASE, STAUROSPORINE, SULFATE ION | | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A. | | Deposit date: | 1999-05-24 | | Release date: | 2000-05-24 | | Last modified: | 2022-12-21 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
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1QPE
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1QPJ
 | | CRYSTAL STRUCTURE OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH STAUROSPORINE. | | Descriptor: | LCK TYROSINE KINASE, STAUROSPORINE, SULFATE ION | | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M. | | Deposit date: | 1999-05-25 | | Release date: | 2000-05-31 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
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1QPC
 | | STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS | | Descriptor: | 1,2-ETHANEDIOL, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, SULFATE ION, ... | | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A. | | Deposit date: | 1999-05-21 | | Release date: | 2000-05-24 | | Last modified: | 2015-08-19 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
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1R0P
 | | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met in complex with the microbial alkaloid K-252a | | Descriptor: | Hepatocyte growth factor receptor, K-252A | | Authors: | Schiering, N, Knapp, S, Marconi, M, Flocco, M.M, Cui, J, Perego, R, Rusconi, L, Cristiani, C. | | Deposit date: | 2003-09-22 | | Release date: | 2003-10-07 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a
Proc.Natl.Acad.Sci.USA, 100, 2003
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1R1W
 | | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET | | Descriptor: | HEPATOCYTE GROWTH FACTOR RECEPTOR | | Authors: | Schiering, N, Knapp, S, Marconi, M, Flocco, M.M, Cui, J, Perego, R, Rusconi, L, Cristiani, C. | | Deposit date: | 2003-09-25 | | Release date: | 2003-10-07 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a
Proc.Natl.Acad.Sci.USA, 100, 2003
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1RJB
 | | Crystal Structure of FLT3 | | Descriptor: | FL cytokine receptor | | Authors: | Griffith, J, Black, J, Faerman, C, Swenson, L, Wynn, M, Lu, F, Lippke, J, Saxena, K. | | Deposit date: | 2003-11-19 | | Release date: | 2004-02-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The structural basis for autoinhibition of FLT3 by the juxtamembrane domain.
Mol.Cell, 13, 2004
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1SNU
 | | CRYSTAL STRUCTURE OF THE UNPHOSPHORYLATED INTERLEUKIN-2 TYROSINE KINASE CATALYTIC DOMAIN | | Descriptor: | STAUROSPORINE, 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: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.
J.Biol.Chem., 279, 2004
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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
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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
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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
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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
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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
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7B8W
 | | Structure of LIMK1 Kinase domain with allosteric inhibitor TH-470 | | Descriptor: | 1,2-ETHANEDIOL, 2-(2-methylpropanoylamino)-~{N}-[2-[(phenylmethyl)-[4-(phenylsulfamoyl)phenyl]carbonyl-amino]ethyl]-1,3-thiazole-5-carboxamide, LIM domain kinase 1 | | Authors: | Lee, H, Yosaatmadja, Y, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Elkins, J.M. | | Deposit date: | 2020-12-13 | | Release date: | 2022-03-02 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structure of LIMK1 Kinase domain with allosteric inhibitor TH-470
To Be Published
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7C2V
 | | Crystal Structure of IRAK4 kinase in complex with the inhibitor CA-4948 | | Descriptor: | 2-(2-methylpyridin-4-yl)-N-[2-morpholin-4-yl-5-[(3R)-3-oxidanylpyrrolidin-1-yl]-[1,3]oxazolo[4,5-b]pyridin-6-yl]-1,3-oxazole-4-carboxamide, Interleukin-1 receptor-associated kinase 4 | | Authors: | Krishnamurthy, N.R, Robert, B. | | Deposit date: | 2020-05-09 | | Release date: | 2020-11-25 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.44 Å) | | Cite: | Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.
Acs Med.Chem.Lett., 11, 2020
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