4D4R
 
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | FOCAL ADHESION KINASE 1, SULFATE ION | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-10-31 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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6GCX
 | | Focal Adhesion Kinase catalytic domain in complex with irreversible inhibitor | | Descriptor: | 2-[[2-[[4-[[[3,4-bis(oxidanylidene)-2-[2-(propanoylamino)ethylamino]cyclobuten-1-yl]amino]methyl]phenyl]amino]-5-chloranyl-pyrimidin-4-yl]amino]-~{N}-methyl-benzamide, Focal adhesion kinase 1, SULFATE ION | | Authors: | Yen-Pon, E, Li, B, Acebron-Garcia de Eulate, M, Tomkiewicz-Raulet, C, Dawson, J, Lietha, D, Frame, M.C, Coumoul, X, Garbay, C, Etheve-Quelquejeu, M, Chen, H. | | Deposit date: | 2018-04-19 | | Release date: | 2019-05-01 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.553 Å) | | Cite: | Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase.
Acs Chem.Biol., 13, 2018
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2JKO
 | | Focal Adhesion Kinase catalytic domain in complex with bis-anilino pyrimidine inhibitor | | Descriptor: | 7-{[(2Z,5S)-5-CHLORO-2-{[2-METHOXY-4-(4-METHYLPIPERAZIN-1-YL)PHENYL]IMINO}-2,5-DIHYDROPYRIMIDIN-4-YL]AMINO}-2-METHYL-2,3-DIHYDRO-1H-ISOINDOL-1-ONE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Eck, M.J. | | Deposit date: | 2008-08-28 | | Release date: | 2008-09-09 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Crystal Structures of the Fak Kinase in Complex with Tae226 and Related Bis-Anilino Pyrimidine Inhibitors Reveal a Helical Dfg Conformation.
Plos One, 3, 2008
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4D5H
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | 6-methyl-5-{[3-(trifluoromethyl)phenyl]amino}-1,2,4-triazin-3(4H)-one, FOCAL ADHESION KINASE 1, SULFATE ION | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-11-05 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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4D5K
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | DIMETHYL SULFOXIDE, FOCAL ADHESION KINASE, SULFATE ION | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-11-05 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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4D4Y
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | DIMETHYL SULFOXIDE, FOCAL ADHESION KINASE 1, SULFATE ION | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-10-31 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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4D58
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6CB0
 | | Crystal Structure of the FAK FERM domain | | Descriptor: | Focal adhesion kinase 1 | | Authors: | Dementiev, A, Marlowe, T. | | Deposit date: | 2018-02-01 | | Release date: | 2019-02-06 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.97 Å) | | Cite: | High resolution crystal structure of the FAK FERM domain reveals new insights on the Druggability of tyrosine 397 and the Src SH3 binding site.
BMC Mol Cell Biol, 20, 2019
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4D4S
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | 2-({5-CHLORO-2-[(2-METHOXY-4-MORPHOLIN-4-YLPHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)-N-METHYLBENZAMIDE, DIMETHYL SULFOXIDE, FOCAL ADHESION KINASE 1, ... | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-10-31 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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2JKK
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6GCW
 | | Focal Adhesion Kinase catalytic domain in complex with irreversible inhibitor | | Descriptor: | 2-[[5-chloranyl-2-[[4-[[[1-[2-(propanoylamino)ethyl]-1,2,3-triazol-4-yl]methylamino]methyl]phenyl]amino]pyrimidin-4-yl]amino]-~{N}-methyl-benzamide, Focal adhesion kinase 1, SULFATE ION | | Authors: | Yen-Pon, E, Li, B, Acebron-Garcia-de-Eulate, M, Tomkiewicz-Raulet, C, Dawson, J, Lietha, D, Frame, M.C, Coumoul, X, Garbay, C, Etheve-Quelquejeu, M, Chen, H. | | Deposit date: | 2018-04-19 | | Release date: | 2019-05-01 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase.
Acs Chem.Biol., 13, 2018
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4BRX
 | | Focal Adhesion Kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor | | Descriptor: | 2-(4-(2-methoxy-4-morpholinophenylamino)-1,3,5-triazin-2-ylamino)-N-methylbenzamide, FOCAL ADHESION KINASE 1, SULFATE ION | | Authors: | Le Coq, J, Lietha, D. | | Deposit date: | 2013-06-05 | | Release date: | 2013-07-24 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Synthesis of Novel Diarylamino-1,3,5-Triazine Derivatives as Fak Inhibitors with Anti-Angiogenic Activity.
Bioorg.Med.Chem.Lett., 23, 2013
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4C7T
 | | Focal Adhesion Kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor | | Descriptor: | FOCAL ADHESION KINASE 1, N-methyl-2-[[4-[(3,4,5-trimethoxyphenyl)amino]-1,3,5-triazin-2-yl]amino]benzamide, SULFATE ION | | Authors: | Le Coq, J, Lietha, D. | | Deposit date: | 2013-09-25 | | Release date: | 2014-04-02 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Inhibition of Both Focal Adhesion Kinase and Fibroblast Growth Factor Receptor 2 Pathways Induces Anti-Tumor and Anti-Angiogenic Activities.
Cancer Lett., 348, 2014
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4D4V
 | | Focal Adhesion Kinase catalytic domain | | Descriptor: | 6-methyl-4-(piperazin-1-yl)-2-(trifluoromethyl)quinoline, DIMETHYL SULFOXIDE, FOCAL ADHESION KINASE, ... | | Authors: | Le Coq, J, Lin, A, Lietha, D. | | Deposit date: | 2014-10-31 | | Release date: | 2015-02-18 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Allosteric Regulation of Focal Adhesion Kinase by Pip2 and ATP.
Biophys.J., 108, 2015
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2J0L
 | | Crystal structure of a the active conformation of the kinase domain of focal adhesion kinase with a phosphorylated activation loop. | | Descriptor: | FOCAL ADHESION KINASE 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-06-26 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase
Cell(Cambridge,Mass.), 129, 2007
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4D55
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6GCR
 | | Focal Adhesion Kinase catalytic domain in complex with irreversible inhibitor | | Descriptor: | 2-[[2-[[4-[[[3,4-bis(oxidanylidene)-2-[2-(propanoylamino)ethylamino]cyclobuten-1-yl]amino]methyl]phenyl]amino]-5-chloranyl-pyrimidin-4-yl]amino]-~{N}-methyl-benzamide, Focal adhesion kinase 1 | | Authors: | Yen-Pon, E, Li, B, Acebron-Garcia de Eulate, M, Tomkiewicz-Raulet, C, Dawson, J, Lietha, D, Frame, M.C, Coumoul, X, Garbay, C, Etheve-Quelquejeu, M, Chen, H. | | Deposit date: | 2018-04-19 | | Release date: | 2019-05-01 | | Last modified: | 2019-10-02 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase.
Acs Chem.Biol., 13, 2018
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2JKM
 | | Focal Adhesion Kinase catalytic domain in complex with bis-anilino pyrimidine inhibitor | | Descriptor: | 2-{[5-CHLORO-2-({(1E,4R)-2-METHOXY-4-[(3R)-3-(METHYLAMINO)PYRROLIDIN-1-YL]CYCLOHEXA-2,5-DIEN-1-YLIDENE}AMINO)PYRIMIDIN-4-YL]AMINO}-N-(1-METHYLETHYL)BENZENESULFONAMIDE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Eck, M.J. | | Deposit date: | 2008-08-28 | | Release date: | 2008-09-09 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Crystal Structures of the Fak Kinase in Complex with Tae226 and Related Bis-Anilino Pyrimidine Inhibitors Reveal a Helical Dfg Conformation.
Plos One, 3, 2008
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2AL6
 | | FERM domain of Focal Adhesion Kinase | | Descriptor: | Focal adhesion kinase 1 | | Authors: | Ceccarelli, D.F, Song, H.K, Poy, F, Schaller, M.D, Eck, M.J. | | Deposit date: | 2005-08-04 | | Release date: | 2005-10-18 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Crystal Structure of the FERM Domain of Focal Adhesion Kinase
J.Biol.Chem., 281, 2006
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2AEH
 | | Focal adhesion kinase 1 | | Descriptor: | Focal adhesion kinase 1 | | Authors: | Ceccarelli, D.F, Song, H.K, Poy, F, Schaller, M.D, Eck, M.J. | | Deposit date: | 2005-07-22 | | Release date: | 2005-10-18 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.53 Å) | | Cite: | Crystal Structure of the FERM Domain of Focal Adhesion Kinase
J.Biol.Chem., 281, 2006
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2JKQ
 | | Focal Adhesion Kinase catalytic domain in complex with bis-anilino pyrimidine inhibitor | | Descriptor: | 4-(1,4'-bipiperidin-1'-yl)-7-({5-chloro-2-[(2-methoxyphenyl)amino]pyrimidin-4-yl}amino)-2-methyl-2,3-dihydro-1H-isoindol-1-one, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Eck, M.J. | | Deposit date: | 2008-08-29 | | Release date: | 2008-09-09 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal Structures of the Fak Kinase in Complex with Tae226 and Related Bis-Anilino Pyrimidine Inhibitors Reveal a Helical Dfg Conformation.
Plos One, 3, 2008
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2J0M
 | | Crystal structure a two-chain complex between the FERM and kinase domains of focal adhesion kinase. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-07-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase.
Cell(Cambridge,Mass.), 129, 2007
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2J0J
 | | Crystal structure of a fragment of focal adhesion kinase containing the FERM and kinase domains. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-06-26 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase
Cell(Cambridge,Mass.), 129, 2007
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2J0K
 | | Crystal structure of a fragment of focal adhesion kinase containing the FERM and kinase domains. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-07-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase.
Cell(Cambridge,Mass.), 129, 2007
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3ZDT
 | | Crystal structure of basic patch mutant FAK FERM domain FAK31- 405 K216A, K218A, R221A, K222A | | Descriptor: | FOCAL ADHESION KINASE 1 | | Authors: | Goni, G.M, Epifano, C, Boskovic, J, Camacho-Artacho, M, Zhou, J, Martin, M.T, Eck, M.J, Kremer, L, Graeter, F, Gervasio, F.L, Perez-Moreno, M, Lietha, D. | | Deposit date: | 2012-11-30 | | Release date: | 2012-12-12 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.15 Å) | | Cite: | Phosphatidylinositol 4,5-Bisphosphate Triggers Activation of Focal Adhesion Kinase by Inducing Clustering and Conformational Changes.
Proc.Natl.Acad.Sci.USA, 111, 2014
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