5B7V
 
 | | Human FGFR1 kinase in complex with CH5183284 | | 分子名称: | Fibroblast growth factor receptor 1, SULFATE ION, [5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl](1H-indol-2-yl)methanone | | 著者 | Fukami, T.A, Lukacs, C.M, Janson, C. | | 登録日 | 2016-06-09 | | 公開日 | 2016-06-22 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor
Mol.Cancer Ther., 13, 2014
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4NKA
 | | Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 2 | | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N~4~-{3-[2-(3,4-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, ... | | 著者 | Norman, R.A, Klein, T. | | 登録日 | 2013-11-12 | | 公開日 | 2013-12-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | | 主引用文献 | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
ACS Med Chem Lett, 5, 2014
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4RWL
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6P69
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6MZW
 | | TAS-120 covalent complex 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, SULFATE ION | | 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 (2.2 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
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5VND
 | | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide, ... | | 著者 | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | | 登録日 | 2017-04-30 | | 公開日 | 2017-05-24 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Cancer Res., 77, 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 | | 分子名称: | 5-(2-thienyl)nicotinic acid, Basic fibroblast growth factor receptor 1, PHOSPHATE ION | | 著者 | Bae, J.H, Ravindranathan, K.P, Mandiyan, V, Ekkati, A.R, Schlessinger, J, Jorgensen, W.L. | | 登録日 | 2009-09-09 | | 公開日 | 2010-02-23 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening
J.Med.Chem., 53, 2010
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5UR1
 | | FGFR1 kinase domain complex with SN37333 in reversible binding mode | | 分子名称: | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{1-[4-(dimethylamino)but-2-enoyl]piperidin-4-yl}-7-(phenylamino)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, Fibroblast growth factor receptor 1 | | 著者 | Yosaatmadja, Y, Paik, W.-K, Smaill, J.B, Squire, C.J. | | 登録日 | 2017-02-09 | | 公開日 | 2017-05-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | 2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.
Eur J Med Chem, 135, 2017
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4F65
 | | Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8 | | 分子名称: | 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, ... | | 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 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.26 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
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6C1O
 | | FGFR1 kinase domain complexed with FIIN-1 | | 分子名称: | Fibroblast growth factor receptor 1, N-(3-{[3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-{[4-(diethylamino)butyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)prop-2-enamide, SULFATE ION | | 著者 | Kalyukina, M, Yosaatmadja, Y, Smaill, J.B, Squire, C.J. | | 登録日 | 2018-01-05 | | 公開日 | 2019-01-16 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.29 Å) | | 主引用文献 | A new class of FGFR1 inhibitors
To Be Published
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4RWI
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6C18
 | | FGFR1 kinase complex with inhibitor SN37115 | | 分子名称: | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{(3S)-1-[(2E)-4-(dimethylamino)but-2-enoyl]pyrrolidin-3-yl}-7-[(propan-2-yl)amino]-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 (2.3 Å) | | 主引用文献 | Understanding the structural requirements for covalent inhibition of FGFR1-3
To Be Published
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5UQ0
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4UWY
 | | FGFR1 Apo structure | | 分子名称: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | | 著者 | Thiyagarajan, N, Bunney, T, Katan, M. | | 登録日 | 2014-08-15 | | 公開日 | 2015-02-25 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.305 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
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4UWB
 | | Fibroblast growth factor receptor 1 kinase in complex with JK-P5 | | 分子名称: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... | | 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 (2.31 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
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4V01
 | | FGFR1 in complex with ponatinib (co-crystallisation). | | 分子名称: | 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 1 (FMS-RELATED TYROSINE KINASE 2, ... | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-09-10 | | 公開日 | 2014-12-10 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4
Structure, 22, 2014
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8XLO
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1AGW
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3KRL
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5Z0S
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4RWJ
 | | Crystal Structure of FGFR1 (C488A, C584S) in complex with AZD4547 (N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE) | | 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 | Sohl, C.D, Anderson, K.S. | | 登録日 | 2014-12-04 | | 公開日 | 2015-04-22 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.489 Å) | | 主引用文献 | Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy.
Acs Chem.Biol., 10, 2015
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7WCL
 | | Crystal structure of FGFR1 kinase domain with Pemigatinib | | 分子名称: | 11-[2,6-bis(fluoranyl)-3,5-dimethoxy-phenyl]-13-ethyl-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.0^{2,6}]trideca-1(9),2(6),3,7-tetraen-12-one, Fibroblast growth factor receptor 1, SULFATE ION | | 著者 | Chen, X.J, Lin, Q.M, Jiang, L.Y, Qu, L.Z, Chen, Y.H. | | 登録日 | 2021-12-20 | | 公開日 | 2022-09-14 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.495 Å) | | 主引用文献 | Characterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants.
Commun Chem, 5, 2022
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5W59
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1FGI
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2FGI
 | | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 | | 分子名称: | 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) | | 著者 | 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. | | 登録日 | 1998-09-15 | | 公開日 | 1999-09-13 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain.
EMBO J., 17, 1998
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