6G54
| Crystal structure of ERK2 covalently bound to SM1-71 | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, Mitogen-activated protein kinase 1, ... | Authors: | Chaikuad, A, Suman, R, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Gray, N.S, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2018-03-29 | Release date: | 2019-02-27 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chem Biol, 26, 2019
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7V29
| Crystal structure of FGFR4 with a dual-warhead covalent inhhibitor | Descriptor: | Fibroblast growth factor receptor 4, N-[2-[[3-(3,5-dimethoxyphenyl)-2-oxidanylidene-1-[3-(4-propanoylpiperazin-1-yl)propyl]-4H-pyrimido[4,5-d]pyrimidin-7-yl]amino]phenyl]propanamide, SULFATE ION | Authors: | Chen, X.J, Jiang, L.Y, Dai, S.Y, Qu, L.Z, Chen, Y.H. | Deposit date: | 2021-08-07 | Release date: | 2022-03-30 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.983 Å) | Cite: | Structure-based design of a dual-warhead covalent inhibitor of FGFR4. Commun Chem, 5, 2022
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3RI1
| Crystal structure of the catalytic domain of FGFR2 kinase in complex with ARQ 069 | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, Fibroblast growth factor receptor 2, SULFATE ION | Authors: | Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A. | Deposit date: | 2011-04-12 | Release date: | 2011-05-04 | Last modified: | 2011-10-19 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. J.Biol.Chem., 286, 2011
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6GES
| Crystal structure of ERK1 covalently bound to SM1-71 | Descriptor: | 1,2-ETHANEDIOL, Mitogen-activated protein kinase 3, N-{2-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino]phenyl}propanamide, ... | Authors: | Chaikuad, A, Suman, R, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Gray, N.S, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2018-04-27 | Release date: | 2019-02-27 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2.07 Å) | Cite: | Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chem Biol, 26, 2019
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8XLQ
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8W1L
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1HKN
| A complex between acidic fibroblast growth factor and 5-amino-2-naphthalenesulfonate | Descriptor: | 5-AMINO-NAPHTALENE-2-MONOSULFONATE, HEPARIN-BINDING GROWTH FACTOR 1 | Authors: | Fernandez-Tornero, C, Lozano, R.M, Gimenez-Gallego, G, Romero, A. | Deposit date: | 2003-03-10 | Release date: | 2004-03-11 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Leads for Development of New Naphthalenesulfonate Derivatives with Enhanced Antiangiogenic Activity: Crystal Structure of Acidic Fibroblast Growth Factor in Complex with 5-Amino-2-Naphthalenesulfonate J.Biol.Chem., 278, 2003
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3OJM
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3OJ2
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7OZY
| FGFR2 kinase domain (residues 461-763) in complex with 38. | Descriptor: | 1,2-ETHANEDIOL, 4-[3-(4-piperazin-4-ium-1-ylphenyl)-1H-indazol-6-yl]phenol, Fibroblast growth factor receptor 2, ... | Authors: | Trinh, C.H, Turner, L.D, Fishwick, C.W.G. | Deposit date: | 2021-06-29 | Release date: | 2021-12-01 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.28 Å) | Cite: | From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor. J.Med.Chem., 65, 2022
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2PSQ
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6ATE
| SRC kinase bound to covalent inhibitor | Descriptor: | N-{2-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino]phenyl}propanamide, Proto-oncogene tyrosine-protein kinase Src | Authors: | Gurbani, D, Westover, K.D. | Deposit date: | 2017-08-28 | Release date: | 2019-02-27 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.402 Å) | Cite: | Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chem Biol, 26, 2019
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4R5S
| Crystal structure of EGFR 696-1022 L858R in complex with FIIN-3 | Descriptor: | Epidermal growth factor receptor, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide | Authors: | Zhu, S.J, Yun, C.H. | Deposit date: | 2014-08-22 | Release date: | 2014-11-12 | Last modified: | 2022-08-24 | Method: | X-RAY DIFFRACTION (3.001 Å) | Cite: | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc.Natl.Acad.Sci.USA, 111, 2014
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4QQC
| Crystal Structure of FGF Receptor (FGFR) 4 Kinase Domain in Complex with FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations | Descriptor: | Fibroblast growth factor receptor 4, N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide, SULFATE ION | Authors: | Huang, Z, Mohammadi, M. | Deposit date: | 2014-06-27 | Release date: | 2014-10-29 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc.Natl.Acad.Sci.USA, 111, 2014
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1E0O
| CRYSTAL STRUCTURE OF A TERNARY FGF1-FGFR2-HEPARIN COMPLEX | Descriptor: | 2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose, FIBROBLAST GROWTH FACTOR 1, FIBROBLAST GROWTH FACTOR RECEPTOR 2, ... | Authors: | Pellegrini, L, Burke, D.F, von Delft, F, Mulloy, B, Blundell, T.L. | Deposit date: | 2000-04-03 | Release date: | 2000-10-23 | Last modified: | 2020-07-29 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Crystal Structure of Fibroblast Growth Factor Receptor Ectodomain Bound to Ligand and Heparin Nature, 407, 2000
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4R6V
| Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex with FIIN-3, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR kinase Gate-Keeper Mutations | Descriptor: | Fibroblast growth factor receptor 4, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide, SULFATE ION | Authors: | Huang, Z, Mohammadi, M. | Deposit date: | 2014-08-26 | Release date: | 2014-10-29 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.353 Å) | Cite: | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc.Natl.Acad.Sci.USA, 111, 2014
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4TYE
| Structural analysis of the human Fibroblast Growth Factor Receptor 4 Kinase | Descriptor: | Fibroblast growth factor receptor 4, PHOSPHATE ION | Authors: | Lesca, E, Lammens, A, Huber, R, Augustin, M. | Deposit date: | 2014-07-08 | Release date: | 2014-09-24 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Structural analysis of the human fibroblast growth factor receptor 4 kinase. J.Mol.Biol., 426, 2014
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4TYJ
| Structural analysis of the human Fibroblast Growth Factor Receptor 4 Kinase | Descriptor: | 1,2-ETHANEDIOL, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide, Fibroblast growth factor receptor 4, ... | Authors: | Lesca, E, Lammens, A, Huber, R, Augustin, M. | Deposit date: | 2014-07-08 | Release date: | 2014-09-24 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (2.45 Å) | Cite: | Structural analysis of the human fibroblast growth factor receptor 4 kinase. J.Mol.Biol., 426, 2014
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4TYG
| Structural analysis of the human Fibroblast Growth Factor Receptor 4 Kinase | Descriptor: | ACETATE ION, Fibroblast growth factor receptor 4 | Authors: | Lesca, E, Lammens, A, Huber, R, Augustin, M. | Deposit date: | 2014-07-08 | Release date: | 2014-09-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structural analysis of the human fibroblast growth factor receptor 4 kinase. J.Mol.Biol., 426, 2014
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4TYI
| Structural analysis of the human Fibroblast Growth Factor Receptor 4 | Descriptor: | 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, Fibroblast growth factor receptor 4 | Authors: | Lesca, E, Lammens, A, Huber, R, Augustin, M. | Deposit date: | 2014-07-08 | Release date: | 2014-09-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (3.4 Å) | Cite: | Structural analysis of the human fibroblast growth factor receptor 4 kinase. J.Mol.Biol., 426, 2014
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6NVJ
| FGFR4 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-fluorophenyl)acrylamide | Descriptor: | Fibroblast growth factor receptor 4, N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-fluorophenyl]propanamide, SULFATE ION | Authors: | Lin, X, Smaill, J.B, Squire, C.J, Yosaatmadja, Y. | Deposit date: | 2019-02-05 | Release date: | 2019-07-10 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. Acs Med.Chem.Lett., 10, 2019
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6NVH
| FGFR4 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide | Descriptor: | Fibroblast growth factor receptor 4, N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide, SULFATE ION | Authors: | Lin, X, Smaill, J.B, Squire, C.J. | Deposit date: | 2019-02-05 | Release date: | 2019-07-10 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. Acs Med.Chem.Lett., 10, 2019
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6NVG
| FGFR4 complex with N-(3,5-dichloro-2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)phenyl)acrylamide | Descriptor: | Fibroblast growth factor receptor 4, N-[3,5-dichloro-2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)phenyl]propanamide, SULFATE ION | Authors: | Lin, X, Smaill, J.B, Squire, C.J, Yosaatmadja, Y. | Deposit date: | 2019-02-05 | Release date: | 2019-07-10 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.99 Å) | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. Acs Med.Chem.Lett., 10, 2019
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6NVK
| FGFR4 complex with BLU-554, N-((3S,4S)-3-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)tetrahydro-2H-pyran-4-yl)acrylamide | Descriptor: | Fibroblast growth factor receptor 4, N-[(3S,4S)-3-{[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino}oxan-4-yl]propanamide, SULFATE ION | Authors: | Lin, X, Smaill, J.B, Squire, C.J, Yosaatmadja, Y. | Deposit date: | 2019-02-05 | Release date: | 2019-07-10 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. Acs Med.Chem.Lett., 10, 2019
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6NVI
| FGFR4 complex with N-(3-chloro-2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-5-fluorophenyl)acrylamide | Descriptor: | Fibroblast growth factor receptor 4, N-[3-chloro-2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-5-fluorophenyl]propanamide, SULFATE ION | Authors: | Lin, X, Smaill, J.B, Squire, C.J, Yosaatmadja, Y. | Deposit date: | 2019-02-05 | Release date: | 2019-07-10 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.117 Å) | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. Acs Med.Chem.Lett., 10, 2019
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