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PDB: 75 件
5EW8
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FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693
分子名称: 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
著者Ogg, D, Breed, J.
登録日2015-11-20
公開日2016-03-30
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (1.63 Å)
主引用文献Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.
Oncotarget, 7, 2016
4WUN
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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
分子名称: 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
著者Squire, C.J, Yosaatmadja, C.J.
登録日2014-11-02
公開日2014-11-19
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (1.65 Å)
主引用文献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
7OZB
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FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 38.
分子名称: 1,2-ETHANEDIOL, 4-[3-(4-piperazin-4-ium-1-ylphenyl)-1H-indazol-6-yl]phenol, Fibroblast growth factor receptor 1, ...
著者Trinh, C.H, Turner, L.D, Fishwick, C.W.G.
登録日2021-06-27
公開日2021-12-01
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.71 Å)
主引用文献From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor.
J.Med.Chem., 65, 2022
8XZ7
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FGFR1 kinase domain with a covalent inhibitor 10h
分子名称: 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
著者Chen, X.J, Chen, Y.H.
登録日2024-01-20
公開日2024-06-26
実験手法X-RAY DIFFRACTION (1.75 Å)
主引用文献Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
7OZD
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FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34.
分子名称: 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]benzamide, ...
著者Trinh, C.H, Turner, L.D, Fishwick, C.W.G.
登録日2021-06-27
公開日2021-12-01
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.82 Å)
主引用文献From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor.
J.Med.Chem., 65, 2022
7OZF
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FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19.
分子名称: 1,2-ETHANEDIOL, CHLORIDE ION, Fibroblast growth factor receptor 1, ...
著者Trinh, C.H, Turner, L.D, Fishwick, C.W.G.
登録日2021-06-28
公開日2021-12-01
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.82 Å)
主引用文献From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor.
J.Med.Chem., 65, 2022
5O49
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Human FGF in complex with a covalent inhibitor
分子名称: 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
著者Debreczeni, J, Breed, J, Mukherjee, H, Aquila, B, Kaiser, C, Tentarelli, S, Whitty, A, Grimster, N.
登録日2017-05-26
公開日2018-02-07
実験手法X-RAY DIFFRACTION (1.91 Å)
主引用文献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
3DPK
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cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor
分子名称: 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, ...
著者Schubert, C.
登録日2008-07-08
公開日2009-02-17
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors
J.Med.Chem., 52, 2009
5AM7
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FGFR1 mutant with an inhibitor
分子名称: 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
著者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.
登録日2015-03-10
公開日2015-03-18
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (1.957 Å)
主引用文献The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study
Ebiomedicine, 2, 2015
4UWC
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Fibroblast growth factor receptor 1 kinase in complex with JK-P3
分子名称: 1,2-ETHANEDIOL, 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ...
著者Beeston, H, Tucker, J, Kankanala, J.
登録日2014-08-11
公開日2015-09-02
最終更新日2024-05-01
実験手法X-RAY DIFFRACTION (1.96 Å)
主引用文献Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Rapid Commun Mass Spectrom, 2021
5AM6
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Native FGFR1 with an inhibitor
分子名称: 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
著者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.
登録日2015-03-10
公開日2015-03-18
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (1.96 Å)
主引用文献The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study
Ebiomedicine, 2, 2015
8JMZ
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FGFR1 kinase domain with sulfatinib
分子名称: 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, ...
著者Chen, X.J, Lin, Q.M, Chen, Y.H.
登録日2023-06-05
公開日2024-03-27
実験手法X-RAY DIFFRACTION (1.988 Å)
主引用文献Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R.
Commun Chem, 7, 2024
6ITJ
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Crystal structure of FGFR1 kinase domain in complex with compound 3
分子名称: 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
著者Xu, Y, Liu, Q.
登録日2018-11-23
公開日2019-10-23
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (1.994 Å)
主引用文献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
6MZQ
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TAS-120 in reversible binding mode with FGFR1
分子名称: 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
著者Kalyukina, M, Squire, C.J.
登録日2018-11-05
公開日2019-01-16
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure.
ChemMedChem, 14, 2019
4ZSA
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BU of 4zsa by Molmil
Crystal structure of FGFR1 kinase domain in complex with 7n
分子名称: 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide, Fibroblast growth factor receptor 1
著者Liu, Q.F, Xu, Y.C.
登録日2015-05-13
公開日2015-06-17
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold.
Org.Biomol.Chem., 13, 2015
1FGK
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1
分子名称: FGF RECEPTOR 1
著者Mohammadi, M, Schlessinger, J, Hubbard, S.R.
登録日1997-02-08
公開日1997-07-23
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism.
Cell(Cambridge,Mass.), 86, 1996
6C1B
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FGFR1 kinase complex with inhibitor SN37118
分子名称: 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
著者Yosaatmadja, Y, Smaill, J.B, Squire, C.J.
登録日2018-01-04
公開日2019-01-16
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
5O4A
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Human FGF in complex with a covalent inhibitor
分子名称: Fibroblast growth factor receptor 1, GLYCEROL, SULFATE ION, ...
著者Debreczeni, J, Breed, J, Mukherjee, H, Aquila, B, Kaiser, C, Tentarelli, S, Whitty, A, Grimster, N.
登録日2017-05-26
公開日2018-02-07
実験手法X-RAY DIFFRACTION (2.01 Å)
主引用文献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
3RHX
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Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069
分子名称: (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, 1,2-ETHANEDIOL, Basic fibroblast growth factor receptor 1, ...
著者Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A.
登録日2011-04-12
公開日2011-05-04
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.01 Å)
主引用文献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
4F64
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Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 6
分子名称: 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, ...
著者Norman, R.A, Breed, J, Ogg, D.
登録日2012-05-14
公開日2012-06-06
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.05 Å)
主引用文献Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.
J.Med.Chem., 55, 2012
3C4F
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FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole
分子名称: 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine, Basic fibroblast growth factor receptor 1
著者Zhang, K.Y.J, Wang, W.
登録日2008-01-29
公開日2008-02-26
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.07 Å)
主引用文献Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
Proc.Natl.Acad.Sci.Usa, 105, 2008
5A4C
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FGFR1 ligand complex
分子名称: 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, ...
著者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.
登録日2015-06-05
公開日2015-08-05
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.09 Å)
主引用文献Structural and Dynamic Insights Into the Energetics of Activation Loop Rearrangement in Fgfr1 Kinase.
Nat.Commun., 6, 2015
3KRJ
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cFMS tyrosine kinase in complex with 4-Cyano-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-yl-phenyl)-amide
分子名称: 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, ...
著者Schubert, C.
登録日2009-11-18
公開日2010-12-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献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
6C19
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FGFR1 kinase complex with inhibitor SN36985
分子名称: 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
著者Yosaatmadja, Y, Smaill, J.B, Squire, C.J.
登録日2018-01-04
公開日2019-01-16
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.12 Å)
主引用文献Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
6C1C
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FGFR1 kinase complex with inhibitor SN37116
分子名称: 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
著者Yosaatmadja, Y, Smaill, J.B, Squire, C.J.
登録日2018-01-04
公開日2019-01-16
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.15 Å)
主引用文献Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published

 

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