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 | 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
|
|
6MZW
| TAS-120 covalent complex 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, SULFATE ION | 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 (2.2 Å) | Cite: | TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure. ChemMedChem, 14, 2019
|
|
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
|
|
2CKN
| |
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
|
|
4NK9
| Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 1 | Descriptor: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N~4~-{5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl}-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, ... | Authors: | Norman, R.A, Klein, T. | Deposit date: | 2013-11-12 | Release date: | 2013-12-18 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.57 Å) | Cite: | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures. ACS Med Chem Lett, 5, 2014
|
|
4NKS
| |
4NKA
| Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 2 | Descriptor: | 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, ... | Authors: | Norman, R.A, Klein, T. | Deposit date: | 2013-11-12 | Release date: | 2013-12-18 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.19 Å) | Cite: | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures. ACS Med Chem Lett, 5, 2014
|
|
4RWL
| |
4RWK
| Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M) in complex with N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE (AZD4547) | Descriptor: | Fibroblast growth factor receptor 1, MAGNESIUM ION, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide | Authors: | Sohl, C.D, Anderson, K.S. | Deposit date: | 2014-12-04 | Release date: | 2015-04-15 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.982 Å) | Cite: | 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
|
|
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) | 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: | Sohl, C.D, Anderson, K.S. | Deposit date: | 2014-12-04 | Release date: | 2015-04-22 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.489 Å) | Cite: | 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
|
|
4RWI
| |
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
|
|
6C1O
| FGFR1 kinase domain complexed with FIIN-1 | Descriptor: | 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 | Authors: | Kalyukina, M, Yosaatmadja, Y, Smaill, J.B, Squire, C.J. | Deposit date: | 2018-01-05 | Release date: | 2019-01-16 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.29 Å) | Cite: | A new class of FGFR1 inhibitors To Be Published
|
|
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
|
|
6C18
| FGFR1 kinase complex with inhibitor SN37115 | Descriptor: | 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 | 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 (2.3 Å) | Cite: | Understanding the structural requirements for covalent inhibition of FGFR1-3 To Be Published
|
|
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
|
|
5A46
| FGFR1 in complex with dovitinib | Descriptor: | 1,2-ETHANEDIOL, 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, 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 | Method: | X-RAY DIFFRACTION (2.63 Å) | Cite: | Structural and Dynamic Insights Into the Energetics of Activation Loop Rearrangement in Fgfr1 Kinase. Nat.Commun., 6, 2015
|
|
4V05
| FGFR1 in complex with AZD4547. | Descriptor: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, PFEIFFER SYNDROME), ... | Authors: | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | Deposit date: | 2014-09-10 | Release date: | 2014-12-10 | Last modified: | 2014-12-17 | Method: | X-RAY DIFFRACTION (2.57 Å) | Cite: | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4 Structure, 22, 2014
|
|
4UWB
| Fibroblast growth factor receptor 1 kinase in complex with JK-P5 | Descriptor: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide, ... | Authors: | Beeston, H, Tucker, J, Kankanala, J. | Deposit date: | 2014-08-11 | Release date: | 2015-09-02 | Last modified: | 2021-06-16 | Method: | X-RAY DIFFRACTION (2.31 Å) | Cite: | Validation of IMS-MS as a screening tool to identify type II kinase inhibitors of FGFR1 kinase. Rapid Commun Mass Spectrom, 2021
|
|
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: | 2021-06-16 | 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
|
|
4V04
| FGFR1 in complex with ponatinib. | Descriptor: | 1,2-ETHANEDIOL, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | Authors: | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | Deposit date: | 2014-09-10 | Release date: | 2014-12-10 | Last modified: | 2018-04-04 | Method: | X-RAY DIFFRACTION (2.12 Å) | Cite: | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4 Structure, 22, 2014
|
|
4V01
| FGFR1 in complex with ponatinib (co-crystallisation). | Descriptor: | 1,2-ETHANEDIOL, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | Authors: | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | Deposit date: | 2014-09-10 | Release date: | 2014-12-10 | Last modified: | 2018-04-04 | Method: | X-RAY DIFFRACTION (2.33 Å) | Cite: | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4 Structure, 22, 2014
|
|
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
|
|
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
|
|