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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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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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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8XLO
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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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4UWY
 | | FGFR1 Apo structure | | Descriptor: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, FIBROBLAST GROWTH FACTOR RECEPTOR 1 | | Authors: | Thiyagarajan, N, Bunney, T, Katan, M. | | Deposit date: | 2014-08-15 | | Release date: | 2015-02-25 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.305 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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6NVL
 | | FGFR1 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide | | Descriptor: | Fibroblast growth factor receptor 1, N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide, SULFATE ION | | Authors: | Lin, X, Smaill, J.B, Squire, C.J. | | Deposit date: | 2019-02-05 | | Release date: | 2019-07-10 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4.
Acs Med.Chem.Lett., 10, 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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5B7V
 | | Human FGFR1 kinase in complex with CH5183284 | | Descriptor: | 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 | | Authors: | Fukami, T.A, Lukacs, C.M, Janson, C. | | Deposit date: | 2016-06-09 | | Release date: | 2016-06-22 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | 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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5Z0S
 | | Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor | | Descriptor: | 1-[(6-chloroimidazo[1,2-b]pyridazin-3-yl)sulfonyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-b]pyridine, Fibroblast growth factor receptor 1 | | Authors: | Liu, Q, Xu, Y. | | Deposit date: | 2017-12-20 | | Release date: | 2018-12-26 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors
Molecules, 23, 2018
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5VND
 | | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | | Descriptor: | 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, ... | | Authors: | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | | Deposit date: | 2017-04-30 | | Release date: | 2017-05-24 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Cancer Res., 77, 2017
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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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7WCL
 | | Crystal structure of FGFR1 kinase domain with Pemigatinib | | Descriptor: | 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 | | Authors: | Chen, X.J, Lin, Q.M, Jiang, L.Y, Qu, L.Z, Chen, Y.H. | | Deposit date: | 2021-12-20 | | Release date: | 2022-09-14 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.495 Å) | | Cite: | Characterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants.
Commun Chem, 5, 2022
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1CVS
 | | CRYSTAL STRUCTURE OF A DIMERIC FGF2-FGFR1 COMPLEX | | Descriptor: | FIBROBLAST GROWTH FACTOR 2, FIBROBLAST GROWTH FACTOR RECEPTOR 1, SULFATE ION | | Authors: | Plotnikov, A.N, Schlessinger, J, Hubbard, S.R, Mohammadi, M. | | Deposit date: | 1999-08-24 | | Release date: | 2000-01-28 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural basis for FGF receptor dimerization and activation.
Cell(Cambridge,Mass.), 98, 1999
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2M49
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5UQ0
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1EVT
 | | CRYSTAL STRUCTURE OF FGF1 IN COMPLEX WITH THE EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) | | Descriptor: | PROTEIN (FIBROBLAST GROWTH FACTOR 1), PROTEIN (FIBROBLAST GROWTH FACTOR RECEPTOR 1), SULFATE ION | | Authors: | Plotnikov, A.N, Hubbard, S.R, Schlessinger, J, Mohammadi, M. | | Deposit date: | 2000-04-20 | | Release date: | 2000-05-31 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structures of two FGF-FGFR complexes reveal the determinants of ligand-receptor specificity.
Cell(Cambridge,Mass.), 101, 2000
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1LWR
 | | Solution structure of the NCAM fibronectin type III module 2 | | Descriptor: | Neural Cell Adhesion Molecule 1, 140 kDa isoform | | Authors: | Kiselyov, V.V, Skladchikova, G, Hinsby, A.M, Jensen, P.H, Kulahin, N, Pedersen, N, Tsetlin, V, Poulsen, F.M, Berezin, V, Bock, E. | | Deposit date: | 2002-06-03 | | Release date: | 2003-06-03 | | Last modified: | 2024-05-22 | | Method: | SOLUTION NMR | | Cite: | Structural basis for a direct interaction between FGFR1 and NCAM and evidence for a regulatory role of ATP
Structure, 11, 2003
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4UXQ
 | | FGFR4 in complex with Ponatinib | | Descriptor: | 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 4, SULFATE ION | | Authors: | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | Deposit date: | 2014-08-27 | | Release date: | 2014-12-03 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.85 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
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1XR0
 | | Structural Basis of SNT PTB Domain Interactions with Distinct Neurotrophic Receptors | | Descriptor: | Basic fibroblast growth factor receptor 1, FGFR signalling adaptor SNT-1 | | Authors: | Dhalluin, C, Yan, K.S, Plotnikova, O, Lee, K.W, Zeng, L, Kuti, M, Mujtaba, S, Goldfarb, M.P, Zhou, M.-M. | | Deposit date: | 2004-10-13 | | Release date: | 2004-11-02 | | Last modified: | 2024-05-22 | | Method: | SOLUTION NMR | | Cite: | Structural Basis of SNT PTB Domain Interactions with Distinct Neurotrophic Receptors
Mol.Cell, 6, 2000
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6P69
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1AGW
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6P68
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3GQI
 | | Crystal Structure of activated receptor tyrosine kinase in complex with substrates | | Descriptor: | Basic fibroblast growth factor receptor 1, DECAVANADATE, MAGNESIUM ION, ... | | Authors: | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | | Deposit date: | 2009-03-24 | | Release date: | 2009-08-18 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.
Cell(Cambridge,Mass.), 138, 2009
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3GQL
 | | Crystal Structure of activated receptor tyrosine kinase in complex with substrates | | Descriptor: | (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol, Basic fibroblast growth factor receptor 1 | | Authors: | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | | Deposit date: | 2009-03-24 | | Release date: | 2009-08-18 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.
Cell(Cambridge,Mass.), 138, 2009
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