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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4X3J
 | | Selection of fragments for kinase inhibitor design: decoration is key | | Descriptor: | 1-[4-(4-amino-5-oxopyrido[2,3-d]pyrimidin-8(5H)-yl)phenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea, Angiopoietin-1 receptor | | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | | Deposit date: | 2014-11-30 | | Release date: | 2014-12-24 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Selection of fragments for kinase inhibitor design: decoration is key.
J.Med.Chem., 58, 2015
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4UWB
 | | Fibroblast growth factor receptor 1 kinase in complex with JK-P5 | | Descriptor: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... | | Authors: | Beeston, H, Tucker, J, Kankanala, J. | | Deposit date: | 2014-08-11 | | Release date: | 2015-09-02 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Rapid Commun Mass Spectrom, 2021
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4UWC
 | | Fibroblast growth factor receptor 1 kinase in complex with JK-P3 | | Descriptor: | 1,2-ETHANEDIOL, 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ... | | Authors: | Beeston, H, Tucker, J, Kankanala, J. | | Deposit date: | 2014-08-11 | | Release date: | 2015-09-02 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.96 Å) | | Cite: | Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Rapid Commun Mass Spectrom, 2021
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4WNM
 | | SYK catalytic domain in complex with a potent triazolopyridine inhibitor | | Descriptor: | N~3~-(tetrahydro-2H-pyran-4-yl)-N~6~-[5-(tetrahydro-2H-pyran-4-ylmethyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]-1H-indazole-3,6-diamine, SULFATE ION, Tyrosine-protein kinase SYK | | Authors: | Jackson, P.J. | | Deposit date: | 2014-10-13 | | Release date: | 2016-01-20 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation.
Plos One, 11, 2016
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4WUN
 | | Structure of FGFR1 in complex with AZD4547 (N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE) at 1.65 angstrom | | Descriptor: | Fibroblast growth factor receptor 1, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide | | Authors: | Squire, C.J, Yosaatmadja, C.J. | | Deposit date: | 2014-11-02 | | Release date: | 2014-11-19 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | The 1.65 angstrom resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition.
Acta Crystallogr.,Sect.D, 71, 2015
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1M17
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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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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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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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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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1M52
 | | Crystal Structure of the c-Abl Kinase domain in complex with PD173955 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 6-(2,6-DICHLORO-PHENYL)-8-METHYL-2-(3-METHYLSULFANYL-PHENYLAMINO)-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1 | | Authors: | Nagar, B, Bornmann, W, Pellicena, P, Schindler, T, Veach, D, Miller, W.T, Clarkson, B, Kuriyan, J. | | Deposit date: | 2002-07-08 | | Release date: | 2002-09-18 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal Structures of the Kinase Domain of c-Abl in Complex with the Small Molecule Inhibitors PD173955 and Imatinib (STI-571)
Cancer Res., 62, 2002
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1MQB
 | | Crystal Structure of Ephrin A2 (ephA2) Receptor Protein Kinase | | Descriptor: | Ephrin type-A receptor 2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | Authors: | Nowakowski, J, Cronin, C.N, McRee, D.E, Knuth, M.W, Nelson, C, Pavletich, N, Rogers, J, Sang, B.C, Scheibe, D.N, Swanson, R.V, Thompson, D.A. | | Deposit date: | 2002-09-16 | | Release date: | 2003-09-16 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structures of the Cancer Related Aurora-A, FAK and EphA2 Protein Kinases from Nanovolume Crystallography
Structure, 10, 2003
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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
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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
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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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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
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1M7N
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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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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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1LUF
 | | Crystal Structure of the MuSK Tyrosine Kinase: Insights into Receptor Autoregulation | | Descriptor: | muscle-specific tyrosine kinase receptor musk | | Authors: | Till, J.H, Becerra, M, Watty, A, Lu, Y, Ma, Y, Neubert, T.A, Burden, S.J, Hubbard, S.R. | | Deposit date: | 2002-05-22 | | Release date: | 2002-09-11 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Crystal structure of the MuSK tyrosine kinase: insights into receptor autoregulation.
Structure, 10, 2002
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7QHG
 | | LIM domain kinase 2 (LIMK2) in complex with 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 2 | | Authors: | Mathea, S, Salah, E, Hanke, T, Knapp, S. | | Deposit date: | 2021-12-12 | | Release date: | 2021-12-22 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
J.Med.Chem., 65, 2022
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7Q7K
 | | JAK2 in complex with 4-(2-amino-8-methoxyquinazolin-6-yl)phenol | | Descriptor: | 4-(2-azanyl-8-methoxy-quinazolin-6-yl)phenol, Tyrosine-protein kinase JAK2 | | Authors: | Rowland, P. | | Deposit date: | 2021-11-09 | | Release date: | 2022-02-02 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.61 Å) | | Cite: | Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
J.Med.Chem., 65, 2022
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