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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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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7OZB
 | | FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S 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 1, ... | | Authors: | Trinh, C.H, Turner, L.D, Fishwick, C.W.G. | | Deposit date: | 2021-06-27 | | Release date: | 2021-12-01 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.71 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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8XZ7
 | | FGFR1 kinase domain with a covalent inhibitor 10h | | Descriptor: | 5-azanyl-3-[2-[4,6-bis(fluoranyl)-2-methyl-3~{H}-benzimidazol-5-yl]ethynyl]-1-[[3-(prop-2-enoylamino)phenyl]methyl]pyrazole-4-carboxamide, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Chen, X.J, Chen, Y.H. | | Deposit date: | 2024-01-20 | | Release date: | 2024-06-26 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
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7OZD
 | | FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34. | | Descriptor: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]benzamide, ... | | Authors: | Trinh, C.H, Turner, L.D, Fishwick, C.W.G. | | Deposit date: | 2021-06-27 | | Release date: | 2021-12-01 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.82 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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7OZF
 | | FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19. | | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, Fibroblast growth factor receptor 1, ... | | Authors: | Trinh, C.H, Turner, L.D, Fishwick, C.W.G. | | Deposit date: | 2021-06-28 | | Release date: | 2021-12-01 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.82 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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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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3DPK
 | | cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor | | Descriptor: | 8-cyclohexyl-N-methoxy-5-oxo-2-{[4-(2-pyrrolidin-1-ylethyl)phenyl]amino}-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, Macrophage colony-stimulating factor 1 receptor, Fibroblast growth factor receptor 1, ... | | Authors: | Schubert, C. | | Deposit date: | 2008-07-08 | | Release date: | 2009-02-17 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors
J.Med.Chem., 52, 2009
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5AM7
 | | FGFR1 mutant with an inhibitor | | Descriptor: | 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, CHLORIDE ION, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | | Authors: | Bunney, T.D, Wan, S, Thiyagarajan, N, Sutto, L, Williams, S.V, Ashford, P, Koss, H, Knowles, M.A, Gervasio, F.L, Coveney, P.V, Katan, M. | | Deposit date: | 2015-03-10 | | Release date: | 2015-03-18 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.957 Å) | | Cite: | The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study
Ebiomedicine, 2, 2015
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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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5AM6
 | | Native FGFR1 with an inhibitor | | Descriptor: | 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, CHLORIDE ION, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | | Authors: | Bunney, T.D, Wan, S, Thiyagarajan, N, Sutto, L, Williams, S.V, Ashford, P, Koss, H, Knowles, M.A, Gervasio, F.L, Coveney, P.V, Katan, M. | | Deposit date: | 2015-03-10 | | Release date: | 2015-03-18 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.96 Å) | | Cite: | The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study
Ebiomedicine, 2, 2015
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8JMZ
 | | FGFR1 kinase domain with sulfatinib | | Descriptor: | Fibroblast growth factor receptor 1, GLYCEROL, N-(2-(dimethylamino)ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)methanesulfonamide, ... | | Authors: | Chen, X.J, Lin, Q.M, Chen, Y.H. | | Deposit date: | 2023-06-05 | | Release date: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (1.988 Å) | | Cite: | Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R.
Commun Chem, 7, 2024
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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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4ZSA
 | | Crystal structure of FGFR1 kinase domain in complex with 7n | | Descriptor: | 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide, Fibroblast growth factor receptor 1 | | Authors: | Liu, Q.F, Xu, Y.C. | | Deposit date: | 2015-05-13 | | Release date: | 2015-06-17 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold.
Org.Biomol.Chem., 13, 2015
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1FGK
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6MZQ
 | | TAS-120 in reversible binding mode with FGFR1 | | Descriptor: | 1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one, Fibroblast growth factor receptor 1 | | Authors: | Kalyukina, M, Squire, C.J. | | Deposit date: | 2018-11-05 | | Release date: | 2019-01-16 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure.
ChemMedChem, 14, 2019
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6C1B
 | | FGFR1 kinase complex with inhibitor SN37118 | | Descriptor: | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{(3S)-1-[(2E)-4-(dimethylamino)but-2-enoyl]pyrrolidin-3-yl}-7-(phenylamino)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, Fibroblast growth factor receptor 1 | | Authors: | Yosaatmadja, Y, Smaill, J.B, Squire, C.J. | | Deposit date: | 2018-01-04 | | Release date: | 2019-01-16 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
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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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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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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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3C4F
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5A4C
 | | FGFR1 ligand complex | | Descriptor: | 1,2-ETHANEDIOL, 1-tert-butyl-3-[2-[3-(diethylamino)propylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | | Authors: | Klein, T, Vajpai, N, Phillips, J.J, Davies, G, Holdgate, G.A, Phillips, C, Tucker, J.A, Norman, R.A, Scott, A.S, Higazi, D.R, Lowe, D, Thompson, G.S, Breeze, A.L. | | Deposit date: | 2015-06-05 | | Release date: | 2015-08-05 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.09 Å) | | Cite: | Structural and Dynamic Insights Into the Energetics of Activation Loop Rearrangement in Fgfr1 Kinase.
Nat.Commun., 6, 2015
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3KRJ
 | | cFMS tyrosine kinase in complex with 4-Cyano-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-yl-phenyl)-amide | | Descriptor: | 4-cyano-N-(2-cyclohex-1-en-1-yl-4-piperidin-4-ylphenyl)-1H-imidazole-2-carboxamide, ACETATE ION, Macrophage colony-stimulating factor 1 receptor, ... | | Authors: | Schubert, C. | | Deposit date: | 2009-11-18 | | Release date: | 2010-12-01 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Optimization of a Potent Class of Arylamide Colony-Stimulating Factor-1 Receptor Inhibitors Leading to Anti-inflammatory Clinical Candidate 4-Cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
J.Med.Chem., 54, 2011
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6C19
 | | FGFR1 kinase complex with inhibitor SN36985 | | Descriptor: | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{(3S)-1-[(2E)-4-(dimethylamino)but-2-enoyl]pyrrolidin-3-yl}-7-(methylamino)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Yosaatmadja, Y, Smaill, J.B, Squire, C.J. | | Deposit date: | 2018-01-04 | | Release date: | 2019-01-16 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
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6C1C
 | | FGFR1 kinase complex with inhibitor SN37116 | | Descriptor: | 7-(cyclohexylamino)-3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{(3S)-1-[(2E)-4-(dimethylamino)but-2-enoyl]pyrrolidin-3-yl}-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Yosaatmadja, Y, Smaill, J.B, Squire, C.J. | | Deposit date: | 2018-01-04 | | Release date: | 2019-01-16 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
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