6ITJ
| Crystal structure of FGFR1 kinase domain in complex with compound 3 | Descriptor: | 4-azanyl-3-(3,5-dimethyl-1-benzofuran-2-yl)-2-phenyl-6~{H}-pyrazolo[3,4-d]pyridazin-7-one, Fibroblast growth factor receptor 1 | Authors: | Xu, Y, Liu, Q. | Deposit date: | 2018-11-23 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.994 Å) | Cite: | Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design. J.Med.Chem., 62, 2019
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5O4A
| Human FGF in complex with a covalent inhibitor | Descriptor: | Fibroblast growth factor receptor 1, GLYCEROL, SULFATE ION, ... | Authors: | Debreczeni, J, Breed, J, Mukherjee, H, Aquila, B, Kaiser, C, Tentarelli, S, Whitty, A, Grimster, N. | Deposit date: | 2017-05-26 | Release date: | 2018-02-07 | Method: | X-RAY DIFFRACTION (2.01 Å) | Cite: | A study of the reactivity of S(VI)-F containing warheads with nucleophilic amino-acid side chains under physiological conditions. Org. Biomol. Chem., 15, 2017
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5O49
| Human FGF in complex with a covalent inhibitor | Descriptor: | Fibroblast growth factor receptor 1, SULFATE ION, [(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl 3-fluorosulfonylbenzoate | Authors: | Debreczeni, J, Breed, J, Mukherjee, H, Aquila, B, Kaiser, C, Tentarelli, S, Whitty, A, Grimster, N. | Deposit date: | 2017-05-26 | Release date: | 2018-02-07 | Method: | X-RAY DIFFRACTION (1.91 Å) | Cite: | A study of the reactivity of S(VI)-F containing warheads with nucleophilic amino-acid side chains under physiological conditions. Org. Biomol. Chem., 15, 2017
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3JS2
| Crystal structure of minimal kinase domain of fibroblast growth factor receptor 1 in complex with 5-(2-thienyl)nicotinic acid | Descriptor: | 5-(2-thienyl)nicotinic acid, Basic fibroblast growth factor receptor 1, PHOSPHATE ION | Authors: | Bae, J.H, Ravindranathan, K.P, Mandiyan, V, Ekkati, A.R, Schlessinger, J, Jorgensen, W.L. | Deposit date: | 2009-09-09 | Release date: | 2010-02-23 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening J.Med.Chem., 53, 2010
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3RHX
| Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, 1,2-ETHANEDIOL, Basic fibroblast growth factor receptor 1, ... | 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: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.01 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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3KXX
| Structure of the mutant Fibroblast Growth Factor receptor 1 | Descriptor: | Basic fibroblast growth factor receptor 1 | Authors: | Bae, J.H, Boggon, T.J, Tome, F, Mandiyan, V, Lax, I, Schlessinger, J. | Deposit date: | 2009-12-04 | Release date: | 2010-03-02 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells. Proc.Natl.Acad.Sci.USA, 107, 2010
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3KY2
| Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain | Descriptor: | Basic fibroblast growth factor receptor 1, SULFATE ION | Authors: | Bae, J.H, Boggon, T.J, Tome, F, Mandiyan, V, Lax, I, Schlessinger, J. | Deposit date: | 2009-12-04 | Release date: | 2010-03-02 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells. Proc.Natl.Acad.Sci.USA, 107, 2010
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1FGI
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5ZV2
| FGFR-1 in complex with ligand lenvatinib | Descriptor: | 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide, Fibroblast growth factor receptor 1 | Authors: | Matsuki, M, Hoshi, T, Yamamoto, Y, Ikemori-Kawada, M, Minoshima, Y, Funahashi, Y, Matsui, J. | Deposit date: | 2018-05-09 | Release date: | 2018-07-11 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.86 Å) | Cite: | Lenvatinib inhibits angiogenesis and tumor fibroblast growth factor signaling pathways in human hepatocellular carcinoma models. Cancer Med, 7, 2018
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3OJV
| Crystal Structure of FGF1 complexed with the ectodomain of FGFR1c exhibiting an ordered ligand specificity-determining betaC'-betaE loop | Descriptor: | 4-deoxy-2-O-sulfo-alpha-L-threo-hex-4-enopyranuronic 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, Basic fibroblast growth factor receptor 1, Heparin-binding growth factor 1 | Authors: | Beenken, A, Mohammadi, M. | Deposit date: | 2010-08-23 | Release date: | 2011-12-28 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Plasticity in Interactions of Fibroblast Growth Factor 1 (FGF1) N Terminus with FGF Receptors Underlies Promiscuity of FGF1. J.Biol.Chem., 287, 2012
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5W59
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7YSH
| Cryo-EM Structure of FGF23-FGFR1c-aKlotho-HS Quaternary Complex | Descriptor: | 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, COPPER (II) ION, Fibroblast growth factor 23, ... | Authors: | Mohammadi, M, Chen, L. | Deposit date: | 2022-08-12 | Release date: | 2023-04-19 | Last modified: | 2023-07-05 | Method: | ELECTRON MICROSCOPY (2.74 Å) | Cite: | Structural basis for FGF hormone signalling. Nature, 618, 2023
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3TT0
| Co-structure of Fibroblast Growth Factor Receptor 1 kinase domain with 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (BGJ398) | Descriptor: | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-1-methylurea, Basic fibroblast growth factor receptor 1, GLYCEROL, ... | Authors: | Bussiere, D.E, Murray, J.M, Shu, W. | Deposit date: | 2011-09-13 | Release date: | 2012-06-13 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J.Med.Chem., 54, 2011
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5EW8
| FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 | Descriptor: | Fibroblast growth factor receptor 1, SULFATE ION, ~{N}'-(3,5-dimethoxyphenyl)-~{N}'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-~{N}-propan-2-yl-ethane-1,2-diamine | Authors: | Ogg, D, Breed, J. | Deposit date: | 2015-11-20 | Release date: | 2016-03-30 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.63 Å) | Cite: | Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use. Oncotarget, 7, 2016
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3C4F
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2CR3
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4F64
| Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 6 | Descriptor: | 1,2-ETHANEDIOL, 5-bromo-N~4~-[3-(3-methoxypropyl)-1H-pyrazol-5-yl]-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1, ... | Authors: | Norman, R.A, Breed, J, Ogg, D. | Deposit date: | 2012-05-14 | Release date: | 2012-06-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase. J.Med.Chem., 55, 2012
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4F63
| Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 1 | Descriptor: | 1,2-ETHANEDIOL, 5-bromo-N~4~-(3-methyl-1H-pyrazol-5-yl)-N~2~-[2-(pyridin-3-yl)ethyl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1 | Authors: | Norman, R.A, Breed, J, Ogg, D. | Deposit date: | 2012-05-14 | Release date: | 2012-06-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase. J.Med.Chem., 55, 2012
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4F65
| Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8 | Descriptor: | 1,2-ETHANEDIOL, 5-bromo-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]-N~4~-[3-(2-phenylethyl)-1H-pyrazol-5-yl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1, ... | Authors: | Norman, R.A, Breed, J, Ogg, D. | Deposit date: | 2012-05-14 | Release date: | 2012-06-06 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.26 Å) | Cite: | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase. J.Med.Chem., 55, 2012
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1FGK
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5FLF
| DISEASE LINKED MUTATION IN FGFR | Descriptor: | ACETATE ION, CHLORIDE ION, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ... | Authors: | Thiyagarajan, N, Bunney, T.D, Katan, M. | Deposit date: | 2015-10-26 | Release date: | 2016-03-30 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.58 Å) | Cite: | Landscape of Activating Cancer Mutations in Fgfr Kinases and Their Differential Responses to Inhibitors in Clinical Use. Oncotarget, 7, 2016
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2FGI
| CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 | Descriptor: | 1-TERT-BUTYL-3-[6-(3,5-DIMETHOXY-PHENYL)-2-(4-DIETHYLAMINO-BUTYLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-YL]-UREA, PROTEIN (FIBROBLAST GROWTH FACTOR (FGF) RECEPTOR 1) | Authors: | Mohammadi, M, Froum, S, Hamby, J.M, Schroeder, M, Panek, R.L, Lu, G.H, Eliseenkova, A.V, Green, D, Schlessinger, J, Hubbard, S.R. | Deposit date: | 1998-09-15 | Release date: | 1999-09-13 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J., 17, 1998
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8JOT
| Crystal structure of CSF-1R kinase domain with sulfatinib | Descriptor: | GLYCEROL, Macrophage colony-stimulating factor 1 receptor, N-(2-(dimethylamino)ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)methanesulfonamide | Authors: | Lin, Q.M, Chen, X.J, Chen, Y.H. | Deposit date: | 2023-06-08 | Release date: | 2024-03-27 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R. Commun Chem, 7, 2024
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7TNH
| Crystal structure of CSF1R kinase domain in complex with DP-6233 | Descriptor: | 2,2-dimethyl-N-[(6-methyl-5-{[2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl]oxy}pyridin-2-yl)carbamoyl]propanamide, CHLORIDE ION, Macrophage colony-stimulating factor 1 receptor,Fibroblast growth factor receptor 1 chimera, ... | Authors: | Edwards, T.E, Arakaki, T.L, Chun, L, Flynn, D.L. | Deposit date: | 2022-01-21 | Release date: | 2022-08-24 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors. Bioorg.Med.Chem.Lett., 74, 2022
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1FQ9
| CRYSTAL STRUCTURE OF A TERNARY FGF2-FGFR1-HEPARIN COMPLEX | Descriptor: | 4-deoxy-2-O-sulfo-alpha-L-threo-hex-4-enopyranuronic 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, 4-deoxy-2-O-sulfo-alpha-L-threo-hex-4-enopyranuronic 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-beta-L-altropyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose, FIBROBLAST GROWTH FACTOR 2, ... | Authors: | Schlessinger, J, Plotnikov, A.N, Ibrahimi, O.A, Eliseenkova, A.V, Yeh, B.K, Yayon, A, Linhardt, R.J, Mohammadi, M. | Deposit date: | 2000-09-04 | Release date: | 2000-09-27 | Last modified: | 2021-11-03 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Crystal structure of a ternary FGF-FGFR-heparin complex reveals a dual role for heparin in FGFR binding and dimerization. Mol.Cell, 6, 2000
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