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5z0s

Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor

Method: X-RAY DIFFRACTION Dmax: 92.5 Å Quality: EXCELLENT
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1. Protein Identity and Related Structures Protein Identity & Related Structures

Fibroblast growth factor receptor 1

Homo sapiens

UniProt P11362

State in the Current Structure

Assembly Oligomeric State Construct Mutations and Modifications Ligands, Ions and Associated Components Method and Experimental Conditions Structure Quality
1 Protein monomer Monomer Protein × 1 PDB declaration: monomeric（1） Consistent with protein copy count Chain A； UniProt 458–765 Fragment：UNP residues 458-765 Mutation：C488A, C584S 960 1-[(6-chloroimidazo[1,2-b]pyridazin-3-yl)sulfonyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-b]pyridine × 1 X-RAY DIFFRACTION X-ray crystallization conditions：VAPOR DIFFUSION, SITTING DROP；pH 6.5；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG Resolution 2.45 Å R-free 0.275
2 Protein monomer Monomer Protein × 1 PDB declaration: monomeric（1） Consistent with protein copy count Chain B； UniProt 458–765 Fragment：UNP residues 458-765 Mutation：C488A, C584S 960 1-[(6-chloroimidazo[1,2-b]pyridazin-3-yl)sulfonyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-b]pyridine × 1 X-RAY DIFFRACTION X-ray crystallization conditions：VAPOR DIFFUSION, SITTING DROP；pH 6.5；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG Resolution 2.45 Å R-free 0.275

Other States of the Same Protein in the Database

Each row is a biological assembly of the same UniProt protein in another PDB entry. The “Difference from current entry” column identifies evidence-level differences; no tag means the currently parsed fields agree.

Other PDB Difference from Current Entry 5Z0S Assembly / Oligomeric State Construct Mutations and Modifications Ligands, Ions and Non-polymers Method and Experimental Conditions Structure Quality
1AGW CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR Deposited 1997-03-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Mutation：L457V, C488A, C584S SU2 3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
Resolution 2.40 Å R-free 0.280
1AGW CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR Deposited 1997-03-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Mutation：L457V, C488A, C584S SU2 3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
Resolution 2.40 Å R-free 0.280
1CVS CRYSTAL STRUCTURE OF A DIMERIC FGF2-FGFR1 COMPLEX Deposited 1999-08-24 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 4 PDB declaration: tetrameric
Chain C 141–365（225 aa） Fragment：IG-LIKE DOMAINS 2 AND 3
Chain D 141–365（225 aa） Fragment：IG-LIKE DOMAINS 2 AND 3
Mutation：YES Mutation：YES SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；ammonium sulfate, glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 2.80 Å R-free 0.281
1CVS CRYSTAL STRUCTURE OF A DIMERIC FGF2-FGFR1 COMPLEX Deposited 1999-08-24 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein heterocomplex Heteromer；Protein × 8 PDB declaration: octameric
Chain C 141–365（225 aa） Fragment：IG-LIKE DOMAINS 2 AND 3
Chain D 141–365（225 aa） Fragment：IG-LIKE DOMAINS 2 AND 3
Mutation：YES Mutation：YES SO4 SULFATE ION × 8 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；ammonium sulfate, glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 2.80 Å R-free 0.281
1EVT CRYSTAL STRUCTURE OF FGF1 IN COMPLEX WITH THE EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) Deposited 2000-04-20 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 4 PDB declaration: tetrameric
Chain C 141–365（225 aa） Fragment：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
Chain D 141–365（225 aa） Fragment：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
Not recorded SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；pH 7.5；298 K；PEG 4000, Isopropanol, HEPES-NaOH, pH 7.5, VAPOR DIFFUSION, temperature 298.0K
Resolution 2.80 Å R-free 0.300
1FGI CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU5402 INHIBITOR Deposited 1997-03-22 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Mutation：L457V, C488A, C584S SU1 3-[(3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-YL)METHYLENE]-2-INDOLINONE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
Resolution 2.50 Å R-free 0.270
1FGI CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU5402 INHIBITOR Deposited 1997-03-22 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Mutation：L457V, C488A, C584S SU1 3-[(3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-YL)METHYLENE]-2-INDOLINONE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
Resolution 2.50 Å R-free 0.270
1FGK CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 Deposited 1997-02-08 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN, HUMAN FGFR1 RESIDUES THAT POSSESS PTK ACTIVITY
Chain B 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN, HUMAN FGFR1 RESIDUES THAT POSSESS PTK ACTIVITY
Mutation：L457V, C488A, C584S Mutation：L457V, C488A, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5
Resolution 2.00 Å R-free 0.261
1FQ9 CRYSTAL STRUCTURE OF A TERNARY FGF2-FGFR1-HEPARIN COMPLEX Deposited 2000-09-04 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 4 PDB declaration: tetrameric
Chain C 141–365（225 aa） Fragment：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
Chain D 141–365（225 aa） Fragment：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
Mutation：N185Q Mutation：N185Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；Ammonium sulfate, Glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 3.00 Å R-free 0.282
1XR0 Structural Basis of SNT PTB Domain Interactions with Distinct Neurotrophic Receptors Deposited 2004-10-13 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 2 PDB declaration: dimeric
Chain A 409–430（22 aa） Fragment：Sequence database residues 409-430 from the juxtamembrane region of hFGFR1
Not recorded No recorded non-water small molecule SOLUTION NMR
NMR measurement conditions pH 6.5；303 K；Ionic strength (raw mmCIF value) 15 mM DTT-d10, and 0.5 mM EDTA00 mM phosphate buffer,；Pressure 1
NMR sample composition SNT-1 PTB domain/hFGFR1 peptide complex (1:1) of ~0.5 mM in 100 mM phosphate buffer of pH 6.5, 5 mM DTT-d10, and 0.5 mM EDTA in H2O/2H2O (9/1) or 2H2O | H2O/2H2O (9/1) or 100% 2H2O
Resolution not provided
2CR3 Solution structure of the first Ig-like domain of human fibroblast growth factor receptor 1 Deposited 2005-05-20 Different construct Different mutation/modification Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 38–123（86 aa） Fragment：Ig domain
Not recorded No recorded non-water small molecule SOLUTION NMR
NMR measurement conditions pH 7；298 K；Ionic strength (raw mmCIF value) 120mM；Pressure ambient
NMR sample composition 1.22mM 13C, 15N-labeled protein; 20mM d-Tris-HCl (pH7.0); 100mM NaCl; 1mM DTT; 0.02% NaN3 | 90% H2O/10% D2O
Resolution not provided
2FGI CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 Deposited 1998-09-15 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Chain B 456–765（310 aa） Fragment：TYROSINE KINASE DOMAIN
Mutation：L457V, C488A, C584S Mutation：L457V, C488A, C584S PD1 1-TERT-BUTYL-3-[6-(3,5-DIMETHOXY-PHENYL)-2-(4-DIETHYLAMINO-BUTYLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-YL]-UREA × 2 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
Resolution 2.50 Å R-free 0.264
3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole Deposited 2008-01-29 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 464–765（302 aa） Fragment：KINASE DOMAIN
Mutation：C488A C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.5；277 K；16% PEG10k, 0.3M (NH4)2SO4, 5% Ethylene Glycol, 100 mM Bis-Tris pH 6.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 2.07 Å R-free 0.264
3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole Deposited 2008-01-29 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 464–765（302 aa） Fragment：KINASE DOMAIN
Mutation：C488A C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.5；277 K；16% PEG10k, 0.3M (NH4)2SO4, 5% Ethylene Glycol, 100 mM Bis-Tris pH 6.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 2.07 Å R-free 0.264
3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole Deposited 2008-01-29 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 464–765（302 aa） Fragment：KINASE DOMAIN
Mutation：C488A C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.5；277 K；16% PEG10k, 0.3M (NH4)2SO4, 5% Ethylene Glycol, 100 mM Bis-Tris pH 6.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 2.07 Å R-free 0.264
3DPK cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor Deposited 2008-07-08 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Monomer；Protein × 1 PDB declaration: monomeric
Chain A 577–597（21 aa） Fragment：KINASE DOMAIN
Mutation：Native kinase insert domain replaced by FGF receptor kinase insert domain SO4 SULFATE ION × 3 8C5 8-cyclohexyl-N-methoxy-5-oxo-2-{[4-(2-pyrrolidin-1-ylethyl)phenyl]amino}-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 5.2；298 K；PEG 3350, SODIUM ACETATE, LI2SO4, pH 5.2, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 1.95 Å R-free 0.244
3GQI Crystal Structure of activated receptor tyrosine kinase in complex with substrates Deposited 2009-03-24 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 2 PDB declaration: dimeric
Chain A 458–774（317 aa） Fragment：Protein kinase domain
Mutation：C488A, Y583F, C584S, Y575F Non-standard monomer：Yes (specific site not provided by mmCIF) DVT DECAVANADATE × 1 ACP PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER × 1 MG MAGNESIUM ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；PEg 8000, taurine, pH 8.0, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.289
3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates Deposited 2009-03-24 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–774（317 aa） Fragment：protein kinase domain
Mutation：C488A GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.289
3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates Deposited 2009-03-24 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–774（317 aa） Fragment：protein kinase domain
Mutation：C488A GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.289
3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates Deposited 2009-03-24 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 458–774（317 aa） Fragment：protein kinase domain
Mutation：C488A GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.289
3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates Deposited 2009-03-24 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–774（317 aa） Fragment：protein kinase domain
Chain B 458–774（317 aa） Fragment：protein kinase domain
Mutation：C488A Mutation：C488A GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 2 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.289
3JS2 Crystal structure of minimal kinase domain of fibroblast growth factor receptor 1 in complex with 5-(2-thienyl)nicotinic acid Deposited 2009-09-09 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：Kinase domain: UNP residues 459-765
Chain B 458–765（308 aa） Fragment：Kinase domain: UNP residues 459-765
Mutation：C488A, C584S Mutation：C488A, C584S VM1 5-(2-thienyl)nicotinic acid × 2 PO4 PHOSPHATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.2M Ammonium sulfate, 0.1M MES pH 6.5, 15% PEG 4000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.20 Å R-free 0.259
3JS2 Crystal structure of minimal kinase domain of fibroblast growth factor receptor 1 in complex with 5-(2-thienyl)nicotinic acid Deposited 2009-09-09 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：Kinase domain: UNP residues 459-765
Chain B 458–765（308 aa） Fragment：Kinase domain: UNP residues 459-765
Mutation：C488A, C584S Mutation：C488A, C584S VM1 5-(2-thienyl)nicotinic acid × 2 PO4 PHOSPHATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.2M Ammonium sulfate, 0.1M MES pH 6.5, 15% PEG 4000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.20 Å R-free 0.259
3KRJ cFMS tyrosine kinase in complex with 4-Cyano-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-yl-phenyl)-amide Deposited 2009-11-18 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Monomer；Protein × 1 PDB declaration: monomeric
Chain A 577–597（21 aa） Fragment：UNP residues 538-678, 753-922
Mutation：C584S ACT ACETATE ION × 1 KRJ 4-cyano-N-(2-cyclohex-1-en-1-yl-4-piperidin-4-ylphenyl)-1H-imidazole-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 5.6；293 K；13-19%PRG3350 100mM NaAcetate, pH 5.6 200mM (NH4)2SO4, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.10 Å R-free 0.260
3KRL cFMS Tyrosine kinase in complex with 5-Cyano-furan-2-carboxylic acid [4-(4-methyl-piperazin-1-yl)-2-piperidin-1-yl-phenyl]-amide Deposited 2009-11-18 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Monomer；Protein × 1 PDB declaration: monomeric
Chain A 577–597（21 aa） Fragment：UNP residues 538-678, 753-922
Mutation：C584S KRL 5-cyano-N-[4-(4-methylpiperazin-1-yl)-2-piperidin-1-ylphenyl]furan-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 5.6；295 K；13-19% PEG3350 100mM NaAc pH 5.6 200mM (NH4)2SO4, VAPOR DIFFUSION, HANGING DROP, temperature 295K
Resolution 2.40 Å R-free 0.264
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 5 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Chain D 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 Deposited 2009-12-04 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 6 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain B 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Chain C 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, R577E, C584S Mutation：C488A, R577E, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；298 K；Crystals were grown at room temperature in 14 days using the hanging drop technique containing equal volumes of protein solution and reservoir buffer (15 % [w/v] polyethylene glycol 3350, 200 mM lithium citrate). , pH 8, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 3.20 Å R-free 0.263
3KY2 Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain Deposited 2009-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, C584S SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.4 M (NH4)2SO4, 15 % PEG 4000, 5 % Glycerol for 1 week., pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.70 Å R-free 0.252
3KY2 Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain Deposited 2009-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Kinase domain (UNP residues 458 to 765)
Mutation：C488A, C584S SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.4 M (NH4)2SO4, 15 % PEG 4000, 5 % Glycerol for 1 week., pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.70 Å R-free 0.252
3OJV Crystal Structure of FGF1 complexed with the ectodomain of FGFR1c exhibiting an ordered ligand specificity-determining betaC'-betaE loop Deposited 2010-08-23 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 2 PDB declaration: dimeric
Chain C 142–365（224 aa） Fragment：FGFR1c
Mutation：N185Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；293 K；0.1M Tris, 15% PEG4000, 0.1M ammonium sulfate, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.60 Å R-free 0.309
3OJV Crystal Structure of FGF1 complexed with the ectodomain of FGFR1c exhibiting an ordered ligand specificity-determining betaC'-betaE loop Deposited 2010-08-23 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein heterocomplex Heteromer；Protein × 2 PDB declaration: dimeric
Chain D 142–365（224 aa） Fragment：FGFR1c
Mutation：N185Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；293 K；0.1M Tris, 15% PEG4000, 0.1M ammonium sulfate, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.60 Å R-free 0.309
3RHX Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 Deposited 2011-04-12 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 461–765（305 aa） Fragment：UNP residues 461-765
Mutation：C488A, C584S 3RH (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine × 1 SO4 SULFATE ION × 1 EDO 1,2-ETHANEDIOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, 0.3M (NH4)2SO4, 5% ethylene glycol, 100mM MES, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.01 Å R-free 0.262
3RHX Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 Deposited 2011-04-12 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 461–765（305 aa） Fragment：UNP residues 461-765
Mutation：C488A, C584S 3RH (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine × 1 EDO 1,2-ETHANEDIOL × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, 0.3M (NH4)2SO4, 5% ethylene glycol, 100mM MES, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.01 Å R-free 0.262
3TT0 Co-structure of Fibroblast Growth Factor Receptor 1 kinase domain with 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (BGJ398) Deposited 2011-09-13 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 456–765（310 aa） Fragment：kinase domain, UNP residues 456-769
Mutation：C584S 07J 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-1-methylurea × 1 SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；CRYSTALLIZED FROM RESERVOIR CONTAINING 18-28% (V:V) PEG-MME 5000, 0.2 M AMSO4, AND 0.1 M SODIUM CACODYLATE , pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.261
3TT0 Co-structure of Fibroblast Growth Factor Receptor 1 kinase domain with 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (BGJ398) Deposited 2011-09-13 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 456–765（310 aa） Fragment：kinase domain, UNP residues 456-769
Mutation：C584S 07J 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-1-methylurea × 1 SO4 SULFATE ION × 1 GOL GLYCEROL × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；CRYSTALLIZED FROM RESERVOIR CONTAINING 18-28% (V:V) PEG-MME 5000, 0.2 M AMSO4, AND 0.1 M SODIUM CACODYLATE , pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.80 Å R-free 0.261
4F63 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 1 Deposited 2012-05-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Chain B 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Mutation：C488A, C584S Mutation：C488A, C584S 0S7 5-bromo-N~4~-(3-methyl-1H-pyrazol-5-yl)-N~2~-[2-(pyridin-3-yl)ethyl]pyrimidine-2,4-diamine × 2 EDO 1,2-ETHANEDIOL × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；16-20% PEG8000, 100 mM PCTP, 100-300 mM ammonium sulfate, 25% ethylene glycol, pH 6.25-7.25, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.55 Å R-free 0.287
4F64 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 6 Deposited 2012-05-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Chain B 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Mutation：C488A, C584S Mutation：C488A, C584S 0S8 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 × 2 EDO 1,2-ETHANEDIOL × 4 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；16-20% PEG8000, 100 mM PCTP, 100-300 mM ammonium sulfate, 25% ethylene glycol, pH 6.25-7.25, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.05 Å R-free 0.269
4F65 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8 Deposited 2012-05-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Chain B 458–765（308 aa） Fragment：kinase domain (UNP residues 458-765)
Mutation：C488A, C584S Mutation：C488A, C584S SO4 SULFATE ION × 4 EDO 1,2-ETHANEDIOL × 10 0S9 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 × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；16-20% PEG8000, 100 mM PCTP, 100-300 mM ammonium sulfate, 25% ethylene glycol, pH 6.25-7.25, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.26 Å R-free 0.235
4NK9 Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 1 Deposited 2013-11-12 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Mutation：YES Mutation：YES EDO 1,2-ETHANEDIOL × 4 SO4 SULFATE ION × 3 2K5 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 × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277.15 K；18-20% PEG 8000, 100mM PCTP, 200mM ammonium sulfate, 25% ethylene glycol, pH 6.75, VAPOR DIFFUSION, HANGING DROP, temperature 277.15K
Resolution 2.57 Å R-free 0.262
4NKA Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 2 Deposited 2013-11-12 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Mutation：C488A, C584S Mutation：C488A, C584S SO4 SULFATE ION × 3 EDO 1,2-ETHANEDIOL × 3 2K7 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 × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277.15 K；18-20% PEG 8000, 100mM PCTP, 200mM ammonium sulfate, 25% ethylene glycol, pH 6.75, VAPOR DIFFUSION, HANGING DROP, temperature 277.15K
Resolution 2.19 Å R-free 0.228
4NKS Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 3 Deposited 2013-11-13 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Mutation：C488A, C584S 2M2 N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]-N~4~-[5-(2-phenylethyl)-1H-pyrazol-3-yl]pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277.15 K；16-20% PEG 8000, 100mM PCTP, 100-300mM ammonium sulfate, 25% ethylene glycol, pH 6.75, VAPOR DIFFUSION, HANGING DROP, temperature 277.15K
Resolution 2.50 Å R-free 0.278
4NKS Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 3 Deposited 2013-11-13 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN (UNP RESIDUES 458-765)
Mutation：C488A, C584S 2M2 N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]-N~4~-[5-(2-phenylethyl)-1H-pyrazol-3-yl]pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277.15 K；16-20% PEG 8000, 100mM PCTP, 100-300mM ammonium sulfate, 25% ethylene glycol, pH 6.75, VAPOR DIFFUSION, HANGING DROP, temperature 277.15K
Resolution 2.50 Å R-free 0.278
4RWI Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M), apo Deposited 2014-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S, V561M No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.4；293 K；0.1 M sodium cacodylate pH 6.4, 30% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.29 Å R-free 0.236
4RWI Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M), apo Deposited 2014-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S, V561M No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.4；293 K；0.1 M sodium cacodylate pH 6.4, 30% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.29 Å R-free 0.236
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) Deposited 2014-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.4；277 K；0.1 M sodium cacodylate pH 6.4, 22% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.49 Å R-free 0.250
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) Deposited 2014-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.4；277 K；0.1 M sodium cacodylate pH 6.4, 22% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.49 Å R-free 0.250
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) Deposited 2014-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S, V561M 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 MG MAGNESIUM ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.6；293 K；0.1 M MES pH 6.6, 34% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.98 Å R-free 0.299
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) Deposited 2014-12-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S, V561M 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.6；293 K；0.1 M MES pH 6.6, 34% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.98 Å R-free 0.299
4RWL Crystal structure of FGFR1 (C488A, C584C) in complex with 6-(7-((1-aminocyclopropyl) methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (E3810) Deposited 2014-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.6；293 K；0.1 M sodium cacodylate pH 6.6, 34% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.19 Å R-free 0.256
4RWL Crystal structure of FGFR1 (C488A, C584C) in complex with 6-(7-((1-aminocyclopropyl) methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (E3810) Deposited 2014-12-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：Residues 458-765
Mutation：C488A, C584S 3ZC 6-({7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl}oxy)-N-methylnaphthalene-1-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.6；293 K；0.1 M sodium cacodylate pH 6.6, 34% PEG 8000, 0.2 M ammonium sulfate, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.19 Å R-free 0.256
4UWB Fibroblast growth factor receptor 1 kinase in complex with JK-P5 Deposited 2014-08-11 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Mutation：YES EDO 1,2-ETHANEDIOL × 3 JVT N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions 20% PEG8000, 20% ETHLYENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
Resolution 2.31 Å R-free 0.272
4UWB Fibroblast growth factor receptor 1 kinase in complex with JK-P5 Deposited 2014-08-11 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Mutation：YES EDO 1,2-ETHANEDIOL × 2 JVT N-[4-(4-methylpiperazin-1-yl)phenyl]-1H-indazole-3-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions 20% PEG8000, 20% ETHLYENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
Resolution 2.31 Å R-free 0.272
4UWC Fibroblast growth factor receptor 1 kinase in complex with JK-P3 Deposited 2014-08-11 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Mutation：YES EDO 1,2-ETHANEDIOL × 7 4Y0 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide × 1 PPI PROPANOIC ACID × 2 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions 20% PEG8000, 20% ETHYLENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
Resolution 1.96 Å R-free 0.206
4UWC Fibroblast growth factor receptor 1 kinase in complex with JK-P3 Deposited 2014-08-11 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Mutation：YES EDO 1,2-ETHANEDIOL × 5 4Y0 3,4-dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)benzamide × 1 PPI PROPANOIC ACID × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions 20% PEG8000, 20% ETHYLENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
Resolution 1.96 Å R-free 0.206
4UWY FGFR1 Apo structure Deposited 2014-08-15 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Not recorded PEG DI(HYDROXYETHYL)ETHER × 1 CL CHLORIDE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 2.31 Å R-free 0.267
4UWY FGFR1 Apo structure Deposited 2014-08-15 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 2.31 Å R-free 0.267
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 Deposited 2014-11-02 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 490–796（307 aa） Fragment：UNP residues 311-490
Not recorded 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 1.65 Å R-free 0.247
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 Deposited 2014-11-02 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 490–796（307 aa） Fragment：UNP residues 311-490
Not recorded 66T N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 1.65 Å R-free 0.247
4ZSA Crystal structure of FGFR1 kinase domain in complex with 7n Deposited 2015-05-13 Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：UNP residues 458-765
Mutation：C488A, C584S 4UT 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
Resolution 2.00 Å R-free 0.254
4ZSA Crystal structure of FGFR1 kinase domain in complex with 7n Deposited 2015-05-13 Different ligand/ion Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：UNP residues 458-765
Mutation：C488A, C584S 4UT 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
Resolution 2.00 Å R-free 0.254
5A4C FGFR1 ligand complex Deposited 2015-06-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 461–765（305 aa） Fragment：RESIDUES 461-765
Mutation：YES SO4 SULFATE ION × 5 EDO 1,2-ETHANEDIOL × 5 XOJ 1-tert-butyl-3-[2-[3-(diethylamino)propylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.09 Å R-free 0.235
5A4C FGFR1 ligand complex Deposited 2015-06-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 461–765（305 aa） Fragment：RESIDUES 461-765
Mutation：YES SO4 SULFATE ION × 1 EDO 1,2-ETHANEDIOL × 5 XOJ 1-tert-butyl-3-[2-[3-(diethylamino)propylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.09 Å R-free 0.235
5AM6 Native FGFR1 with an inhibitor Deposited 2015-03-10 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Not recorded CL CHLORIDE ION × 3 38O 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 1.96 Å R-free 0.252
5AM6 Native FGFR1 with an inhibitor Deposited 2015-03-10 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, RESIDUES 458-765
Not recorded 38O 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 1.96 Å R-free 0.252
5AM7 FGFR1 mutant with an inhibitor Deposited 2015-03-10 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES 38O 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one × 1 CL CHLORIDE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 1.96 Å R-free 0.254
5AM7 FGFR1 mutant with an inhibitor Deposited 2015-03-10 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES 38O 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one × 1 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
Resolution 1.96 Å R-free 0.254
5B7V Human FGFR1 kinase in complex with CH5183284 Deposited 2016-06-09 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 456–765（310 aa） Fragment：tyrosine kinase domain, UNP residues 456-765
Mutation：L457V, C488A, C584S LWJ [5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl](1H-indol-2-yl)methanone × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, (NH4)2SO4, BIS-TRIS
Resolution 2.15 Å R-free 0.256
5B7V Human FGFR1 kinase in complex with CH5183284 Deposited 2016-06-09 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 456–765（310 aa） Fragment：tyrosine kinase domain, UNP residues 456-765
Mutation：L457V, C488A, C584S LWJ [5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl](1H-indol-2-yl)methanone × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, (NH4)2SO4, BIS-TRIS
Resolution 2.15 Å R-free 0.256
5EW8 FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 Deposited 2015-11-20 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded SO4 SULFATE ION × 2 5SF ~{N}'-(3,5-dimethoxyphenyl)-~{N}'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-~{N}-propan-2-yl-ethane-1,2-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277 K；18-20% PEG8000, 200mM Ammonium sulphate, 100mM PCTP, 20% (v/v) ethylene glycol
Resolution 1.63 Å R-free 0.206
5EW8 FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 Deposited 2015-11-20 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded SO4 SULFATE ION × 1 5SF ~{N}'-(3,5-dimethoxyphenyl)-~{N}'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-~{N}-propan-2-yl-ethane-1,2-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.75；277 K；18-20% PEG8000, 200mM Ammonium sulphate, 100mM PCTP, 20% (v/v) ethylene glycol
Resolution 1.63 Å R-free 0.206
5FLF DISEASE LINKED MUTATION IN FGFR Deposited 2015-10-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES SO4 SULFATE ION × 1 ACT ACETATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
Resolution 2.58 Å R-free 0.255
5FLF DISEASE LINKED MUTATION IN FGFR Deposited 2015-10-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES SO4 SULFATE ION × 1 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
Resolution 2.58 Å R-free 0.255
5FLF DISEASE LINKED MUTATION IN FGFR Deposited 2015-10-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES SO4 SULFATE ION × 1 CL CHLORIDE ION × 1 PGE TRIETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
Resolution 2.58 Å R-free 0.255
5FLF DISEASE LINKED MUTATION IN FGFR Deposited 2015-10-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES SO4 SULFATE ION × 5 CL CHLORIDE ION × 3 PGE TRIETHYLENE GLYCOL × 3 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
Resolution 2.58 Å R-free 0.255
5FLF DISEASE LINKED MUTATION IN FGFR Deposited 2015-10-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 5 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain E 458–765（308 aa） Fragment：KINASE DOMAIN, UNP RESIDUES 458-765
Mutation：YES SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
Resolution 2.58 Å R-free 0.255
5O49 Human FGF in complex with a covalent inhibitor Deposited 2017-05-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Not recorded 9K5 [(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl 3-fluorosulfonylbenzoate × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；277 K；18-20% (w/v) PEG8000, 200mM ammonium sulphate, 100mM PCTP pH 6.75 and 20% (v/v) ethylene glycol
Resolution 1.91 Å R-free 0.220
5O49 Human FGF in complex with a covalent inhibitor Deposited 2017-05-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Not recorded 9K5 [(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl 3-fluorosulfonylbenzoate × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；277 K；18-20% (w/v) PEG8000, 200mM ammonium sulphate, 100mM PCTP pH 6.75 and 20% (v/v) ethylene glycol
Resolution 1.91 Å R-free 0.220
5O4A Human FGF in complex with a covalent inhibitor Deposited 2017-05-26 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded SO4 SULFATE ION × 2 GOL GLYCEROL × 1 9K8 [(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl 4-ethyl-3-fluorosulfonyl-benzoate × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18-20% (w/v) PEG8000, 200mM ammonium sulphate, 100mM PCTP pH 6.75 and 20% (v/v) ethylene glycol
Resolution 2.01 Å R-free 0.225
5O4A Human FGF in complex with a covalent inhibitor Deposited 2017-05-26 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded SO4 SULFATE ION × 1 9K8 [(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl 4-ethyl-3-fluorosulfonyl-benzoate × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18-20% (w/v) PEG8000, 200mM ammonium sulphate, 100mM PCTP pH 6.75 and 20% (v/v) ethylene glycol
Resolution 2.01 Å R-free 0.225
5UQ0 FGFR1 kinase domain complex with fragment 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxamide Deposited 2017-02-05 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C488A, C584S WP1 2,2-dimethyl-2,3-dihydro-1-benzofuran-7-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.30 Å R-free 0.294
5UQ0 FGFR1 kinase domain complex with fragment 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxamide Deposited 2017-02-05 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C488A, C584S WP1 2,2-dimethyl-2,3-dihydro-1-benzofuran-7-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.30 Å R-free 0.294
5UR1 FGFR1 kinase domain complex with SN37333 in reversible binding mode Deposited 2017-02-09 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa）
Mutation：C488A, C584S YY9 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.20 Å R-free 0.277
5UR1 FGFR1 kinase domain complex with SN37333 in reversible binding mode Deposited 2017-02-09 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa）
Mutation：C488A, C584S YY9 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.20 Å R-free 0.277
5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 Deposited 2017-04-30 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 456–763（308 aa） Fragment：unp residues 458-765
Mutation：C486A, Y561C, C582S 9ES N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide × 1 SO4 SULFATE ION × 2 EDO 1,2-ETHANEDIOL × 9 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
Resolution 2.20 Å R-free 0.223
5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 Deposited 2017-04-30 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 456–763（308 aa） Fragment：unp residues 458-765
Mutation：C486A, Y561C, C582S 9ES N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide × 1 SO4 SULFATE ION × 2 EDO 1,2-ETHANEDIOL × 6 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
Resolution 2.20 Å R-free 0.223
5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 Deposited 2017-04-30 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 456–763（308 aa） Fragment：unp residues 458-765
Chain B 456–763（308 aa） Fragment：unp residues 458-765
Mutation：C486A, Y561C, C582S Mutation：C486A, Y561C, C582S 9ES N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide × 2 SO4 SULFATE ION × 4 EDO 1,2-ETHANEDIOL × 15 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
Resolution 2.20 Å R-free 0.223
5W21 Crystal Structure of a 1:1:1 FGF23-FGFR1c-aKlotho Ternary Complex Deposited 2017-06-05 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 3 PDB declaration: trimeric
Chain C 142–365（224 aa） Fragment：D2 and D3 region (UNP residues 142-365)
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 7 ZN ZINC ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；22% PEG350 MME, 0.1 M Tris-HCl, pH 8.0, 1 mM reduced glutathione, 1 mM oxidized glutathione
Resolution 3.00 Å R-free 0.278
5W59 Crystal structure of a monomeric human FGF9 in complex with the ectodomain of human FGFR1c Deposited 2017-06-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 2 PDB declaration: dimeric
Chain B 142–365（224 aa） Fragment：;Extracellular ligand binding domain of the "c" splice isoform (UNP residues 142-365) ;
Not recorded SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；291 K；100 mM Tris, pH 8.0, 8% w/v PEG20000, 0.3 M sodium chloride, 40 mM L-proline
Resolution 2.50 Å R-free 0.221
5ZV2 FGFR-1 in complex with ligand lenvatinib Deposited 2018-05-09 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 461–764（304 aa） Fragment：KINASE DOMAIN
Mutation：C488A LEV 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；pH 7；277 K；17.70 % PEG-5000-MME, 0.20 M (NH4)2SO4, 0.10 M Tris pH 7.00, Cryo 25% Ethylenglycole in reservoir solution.
Resolution 2.86 Å R-free 0.269
5ZV2 FGFR-1 in complex with ligand lenvatinib Deposited 2018-05-09 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 461–764（304 aa） Fragment：KINASE DOMAIN
Mutation：C488A LEV 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；pH 7；277 K；17.70 % PEG-5000-MME, 0.20 M (NH4)2SO4, 0.10 M Tris pH 7.00, Cryo 25% Ethylenglycole in reservoir solution.
Resolution 2.86 Å R-free 0.269
6C18 FGFR1 kinase complex with inhibitor SN37115 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY5 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 × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.30 Å R-free 0.267
6C18 FGFR1 kinase complex with inhibitor SN37115 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY5 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.30 Å R-free 0.267
6C19 FGFR1 kinase complex with inhibitor SN36985 Deposited 2018-01-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa）
Mutation：C488A, C584S YY7 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 × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.12 Å R-free 0.239
6C19 FGFR1 kinase complex with inhibitor SN36985 Deposited 2018-01-04 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa）
Mutation：C488A, C584S YY7 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.12 Å R-free 0.239
6C1B FGFR1 kinase complex with inhibitor SN37118 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY4 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.00 Å R-free 0.255
6C1B FGFR1 kinase complex with inhibitor SN37118 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY4 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.00 Å R-free 0.255
6C1C FGFR1 kinase complex with inhibitor SN37116 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY6 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.15 Å R-free 0.270
6C1C FGFR1 kinase complex with inhibitor SN37116 Deposited 2018-01-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa） Fragment：UNP residues 457-763
Mutation：C486A, C582S YY6 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 × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.15 Å R-free 0.270
6C1O FGFR1 kinase domain complexed with FIIN-1 Deposited 2018-01-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 457–763（307 aa）
Not recorded MK9 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 × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.29 Å R-free 0.276
6C1O FGFR1 kinase domain complexed with FIIN-1 Deposited 2018-01-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 457–763（307 aa）
Not recorded MK9 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
Resolution 2.29 Å R-free 0.276
6ITJ Crystal structure of FGFR1 kinase domain in complex with compound 3 Deposited 2018-11-23 Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa） Fragment：UNP residues 458-765
Mutation：C488A, C584S AXU 4-azanyl-3-(3,5-dimethyl-1-benzofuran-2-yl)-2-phenyl-6~{H}-pyrazolo[3,4-d]pyridazin-7-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
Resolution 1.99 Å R-free 0.244
6ITJ Crystal structure of FGFR1 kinase domain in complex with compound 3 Deposited 2018-11-23 Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa） Fragment：UNP residues 458-765
Mutation：C488A, C584S AXU 4-azanyl-3-(3,5-dimethyl-1-benzofuran-2-yl)-2-phenyl-6~{H}-pyrazolo[3,4-d]pyridazin-7-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
Resolution 1.99 Å R-free 0.244
6MZQ TAS-120 in reversible binding mode with FGFR1 Deposited 2018-11-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 368–674（307 aa）
Not recorded TZ0 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, sodium cacodylate, ammonium sulfate
Resolution 2.00 Å R-free 0.230
6MZQ TAS-120 in reversible binding mode with FGFR1 Deposited 2018-11-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 368–674（307 aa）
Not recorded TZ0 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, sodium cacodylate, ammonium sulfate
Resolution 2.00 Å R-free 0.230
6MZW TAS-120 covalent complex with FGFR1 Deposited 2018-11-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 368–674（307 aa）
Not recorded TZ0 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 × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, ammonium sulfate, sodium cacodylate
Resolution 2.20 Å R-free 0.297
6MZW TAS-120 covalent complex with FGFR1 Deposited 2018-11-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 368–674（307 aa）
Not recorded TZ0 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, ammonium sulfate, sodium cacodylate
Resolution 2.20 Å R-free 0.297
6NVL FGFR1 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide Deposited 2019-02-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C584S SO4 SULFATE ION × 1 XL6 N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 7.5；291 K；90 mM NPS salt mixture (30 mM sodium nitrate, 30 mM sodium phosphate dibasic, 30 mM ammonium sulfatesulfate), 100 mM HEPES/MOPS pH 7.5, and 50% v/v of a precipitant mixture of 40% v/v PEG 500 MME and 20 % w/v PEG 20,000
Resolution 2.70 Å R-free 0.263
6NVL FGFR1 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide Deposited 2019-02-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C584S SO4 SULFATE ION × 1 XL6 N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 7.5；291 K；90 mM NPS salt mixture (30 mM sodium nitrate, 30 mM sodium phosphate dibasic, 30 mM ammonium sulfatesulfate), 100 mM HEPES/MOPS pH 7.5, and 50% v/v of a precipitant mixture of 40% v/v PEG 500 MME and 20 % w/v PEG 20,000
Resolution 2.70 Å R-free 0.263
6NVL FGFR1 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide Deposited 2019-02-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 458–765（308 aa）
Mutation：C584S XL6 N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 7.5；291 K；90 mM NPS salt mixture (30 mM sodium nitrate, 30 mM sodium phosphate dibasic, 30 mM ammonium sulfatesulfate), 100 mM HEPES/MOPS pH 7.5, and 50% v/v of a precipitant mixture of 40% v/v PEG 500 MME and 20 % w/v PEG 20,000
Resolution 2.70 Å R-free 0.263
6NVL FGFR1 complex with N-(2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-3-methylphenyl)acrylamide Deposited 2019-02-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 458–765（308 aa）
Mutation：C584S SO4 SULFATE ION × 3 XL6 N-[2-({5-[(2,6-dichloro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl}amino)-3-methylphenyl]propanamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 7.5；291 K；90 mM NPS salt mixture (30 mM sodium nitrate, 30 mM sodium phosphate dibasic, 30 mM ammonium sulfatesulfate), 100 mM HEPES/MOPS pH 7.5, and 50% v/v of a precipitant mixture of 40% v/v PEG 500 MME and 20 % w/v PEG 20,000
Resolution 2.70 Å R-free 0.263
6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. Deposited 2019-06-03 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：Y563C,C488A O1Y N-{3-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-1-(2-hydroxyethyl)-1H-pyrazol-4-yl}prop-2-enamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；1:1 mix of protein + reservoir Protein at ~15 mg/mL formulated in: 20mM Tris pH 8, 20mM NaCl, 2mM TCEP Reservoir: 14-18% PEG 10K 0.3 M (NH4)2SO4 0.1 M MES pH 6.5 5% ethylene glycol
Resolution 2.90 Å R-free 0.303
6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. Deposited 2019-06-03 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：Y563C,C488A O1Y N-{3-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-1-(2-hydroxyethyl)-1H-pyrazol-4-yl}prop-2-enamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；1:1 mix of protein + reservoir Protein at ~15 mg/mL formulated in: 20mM Tris pH 8, 20mM NaCl, 2mM TCEP Reservoir: 14-18% PEG 10K 0.3 M (NH4)2SO4 0.1 M MES pH 6.5 5% ethylene glycol
Resolution 2.90 Å R-free 0.303
6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. Deposited 2019-06-03 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 458–765（308 aa）
Mutation：Y563C,C488A O1Y N-{3-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-1-(2-hydroxyethyl)-1H-pyrazol-4-yl}prop-2-enamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；1:1 mix of protein + reservoir Protein at ~15 mg/mL formulated in: 20mM Tris pH 8, 20mM NaCl, 2mM TCEP Reservoir: 14-18% PEG 10K 0.3 M (NH4)2SO4 0.1 M MES pH 6.5 5% ethylene glycol
Resolution 2.90 Å R-free 0.303
6P69 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 11. Deposited 2019-06-03 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C488A, Y563C SO4 SULFATE ION × 1 EDO 1,2-ETHANEDIOL × 2 O21 N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl][3-(4-methylpiperazin-1-yl)propyl]amino}pyrimidin-4-yl)amino]phenyl}prop-2-enamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；1:1 mix of protein + reservoir Protein at ~15 mg/mL formulated in: 20mM Tris pH 8, 20mM NaCl, 2mM TCEP Reservoir: 14-18% PEG 10K 0.3 M (NH4)2SO4 0.1 M MES pH 6.5 5% ethylene glycol
Resolution 2.20 Å R-free 0.245
6P69 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 11. Deposited 2019-06-03 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C488A, Y563C SO4 SULFATE ION × 2 EDO 1,2-ETHANEDIOL × 1 O21 N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl][3-(4-methylpiperazin-1-yl)propyl]amino}pyrimidin-4-yl)amino]phenyl}prop-2-enamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；1:1 mix of protein + reservoir Protein at ~15 mg/mL formulated in: 20mM Tris pH 8, 20mM NaCl, 2mM TCEP Reservoir: 14-18% PEG 10K 0.3 M (NH4)2SO4 0.1 M MES pH 6.5 5% ethylene glycol
Resolution 2.20 Å R-free 0.245
7OZB FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 38. Deposited 2021-06-27 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 47I 4-[3-(4-piperazin-4-ium-1-ylphenyl)-1H-indazol-6-yl]phenol × 1 SO4 SULFATE ION × 2 EDO 1,2-ETHANEDIOL × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.71 Å R-free 0.244
7OZB FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 38. Deposited 2021-06-27 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain BBB 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 47I 4-[3-(4-piperazin-4-ium-1-ylphenyl)-1H-indazol-6-yl]phenol × 1 SO4 SULFATE ION × 3 EDO 1,2-ETHANEDIOL × 5 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.71 Å R-free 0.244
7OZD FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34. Deposited 2021-06-27 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 42I N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]benzamide × 1 SO4 SULFATE ION × 5 EDO 1,2-ETHANEDIOL × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.82 Å R-free 0.241
7OZD FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34. Deposited 2021-06-27 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain BBB 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 42I N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]benzamide × 1 SO4 SULFATE ION × 3 EDO 1,2-ETHANEDIOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.82 Å R-free 0.241
7OZF FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19. Deposited 2021-06-28 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 466 N-[6-(3-ethoxyphenyl)-1H-indazol-3-yl]benzamide × 1 SO4 SULFATE ION × 1 EDO 1,2-ETHANEDIOL × 2 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.82 Å R-free 0.242
7OZF FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19. Deposited 2021-06-28 Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain BBB 458–765（308 aa） Fragment：UNP residues 458-765
Not recorded 466 N-[6-(3-ethoxyphenyl)-1H-indazol-3-yl]benzamide × 1 EDO 1,2-ETHANEDIOL × 2 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.7；291 K；0.185M ammonium sulfate, 20% v/v ethylene glycol, 17% w/v PEG 8000, 0.1M PCPT
Resolution 1.82 Å R-free 0.242
7TNH Crystal structure of CSF1R kinase domain in complex with DP-6233 Deposited 2022-01-21 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Monomer；Protein × 1 PDB declaration: monomeric
Chain A 577–597（21 aa）
Not recorded NA SODIUM ION × 1 CL CHLORIDE ION × 4 I9W 2,2-dimethyl-N-[(6-methyl-5-{[2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl]oxy}pyridin-2-yl)carbamoyl]propanamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 6.5；295 K；CSF1R at 10.7 mg/mL in 50 mM Tris pH 7.5, 200 mM NaCl, 5% glycerol with 5-fold excess of arylamide compound against 10% PEG 10,000, 0.1 M MES pH 6.5 and 0.1 M magnesium acetate soaked over two nights with 1 mM DP-6233 and 20% ethylene glycol as cryo
Resolution 2.70 Å R-free 0.269
7WCL Crystal structure of FGFR1 kinase domain with Pemigatinib Deposited 2021-12-20 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C584S 8ZF 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 × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277.15 K；18% (w/v) PEG 8000, 0.2 M LiSO4, 0.1 M MES (pH 6.5)
Resolution 2.50 Å R-free 0.230
7WCL Crystal structure of FGFR1 kinase domain with Pemigatinib Deposited 2021-12-20 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C584S 8ZF 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 × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；277.15 K；18% (w/v) PEG 8000, 0.2 M LiSO4, 0.1 M MES (pH 6.5)
Resolution 2.50 Å R-free 0.230
8JMZ FGFR1 kinase domain with sulfatinib Deposited 2023-06-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C129S UKI Sulfatinib × 1 SO4 SULFATE ION × 6 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；0.1 M MES pH 6.6,34% PEG 8000,0.2 M ammonium sulfate
Resolution 1.99 Å R-free 0.205
8JMZ FGFR1 kinase domain with sulfatinib Deposited 2023-06-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C129S UKI Sulfatinib × 1 SO4 SULFATE ION × 3 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；0.1 M MES pH 6.6,34% PEG 8000,0.2 M ammonium sulfate
Resolution 1.99 Å R-free 0.205
8JQI Cryo EM map of full length PLC gamma 2 and FGFR1 Kinase Domain Deposited 2023-06-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Protein heterocomplex Heteromer；Protein × 2 PDB declaration: dimeric
Chain B 1–822（822 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 7.9；25 mM Tris pH 7.9, 150 mM NaCl, 1mM TCEP
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 4.10 Å
8XLO FGFR1 kinase domain with a dual-warhead covalent inhibitor CXF-007 Deposited 2023-12-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C584S A1LVQ CXF007 × 1 SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 2.36 Å R-free 0.255
8XLO FGFR1 kinase domain with a dual-warhead covalent inhibitor CXF-007 Deposited 2023-12-26 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C584S A1LVQ CXF007 × 1 SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 2.36 Å R-free 0.255
8XZ7 FGFR1 kinase domain with a covalent inhibitor 10h Deposited 2024-01-20 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C129S SO4 SULFATE ION × 3 A1LWW 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 1.75 Å R-free 0.225
8XZ7 FGFR1 kinase domain with a covalent inhibitor 10h Deposited 2024-01-20 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C129S SO4 SULFATE ION × 2 A1LWW 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 × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 1.75 Å R-free 0.225
8Y22 FGFR1 kinase domain with a covalent inhibitor 9g Deposited 2024-01-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C127S A1LW9 ~{N}-[4-[[4-azanyl-3-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]propanamide × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 2.79 Å R-free 0.260
8Y22 FGFR1 kinase domain with a covalent inhibitor 9g Deposited 2024-01-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C127S A1LW9 ~{N}-[4-[[4-azanyl-3-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]propanamide × 1 SO4 SULFATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 2.79 Å R-free 0.260
8YKI FGFR-1 in complex with ligand tasurgratinib Deposited 2024-03-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 461–774（314 aa）
Mutation：C488A A1LY1 Tasurgratinib × 1 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；293 K；18% w/v PEG 3350, 0.2M (NH4)2 TARTRATE
Resolution 2.79 Å R-free 0.288
8YKI FGFR-1 in complex with ligand tasurgratinib Deposited 2024-03-05 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 461–774（314 aa）
Mutation：C488A A1LY1 Tasurgratinib × 1 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；293 K；18% w/v PEG 3350, 0.2M (NH4)2 TARTRATE
Resolution 2.79 Å R-free 0.288
9CD5 FGFR1 Kinase Domain Soak with Inhibitor TYRA-300 Deposited 2024-06-24 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Mutation：C488A, C584S EDO 1,2-ETHANEDIOL × 2 A1AV2 (3P)-5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-3-{6-[6-(methanesulfonyl)-2,6-diazaspiro[3.3]heptan-2-yl]pyridin-3-yl}-1H-indazole × 1 SO4 SULFATE ION × 9 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；25%P8K, 25% EG, 0.25M AS, 0.1MPCTP pH7.5
Resolution 2.94 Å R-free 0.263
9CD5 FGFR1 Kinase Domain Soak with Inhibitor TYRA-300 Deposited 2024-06-24 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Mutation：C488A, C584S EDO 1,2-ETHANEDIOL × 1 A1AV2 (3P)-5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-3-{6-[6-(methanesulfonyl)-2,6-diazaspiro[3.3]heptan-2-yl]pyridin-3-yl}-1H-indazole × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；25%P8K, 25% EG, 0.25M AS, 0.1MPCTP pH7.5
Resolution 2.94 Å R-free 0.263
9U7G FGFR1 kinase domain with a macrocyclic compound 8g Deposited 2025-03-24 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Not recorded A1EOH (E)-4-methyl-17-(1-methyl-1H-pyrazol-4-yl)-7,10-dioxa-4-aza-1(3,6)-imidazo[1,2-b]pyridazina-2(3,5)-pyridinacyclodecaphan-3-one × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；20% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.66 Å R-free 0.216
9U7G FGFR1 kinase domain with a macrocyclic compound 8g Deposited 2025-03-24 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Not recorded A1EOH (E)-4-methyl-17-(1-methyl-1H-pyrazol-4-yl)-7,10-dioxa-4-aza-1(3,6)-imidazo[1,2-b]pyridazina-2(3,5)-pyridinacyclodecaphan-3-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；20% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.66 Å R-free 0.216
9UHC FGFR1 kinase domain with a covalent inhibitor 9p Deposited 2025-04-14 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Not recorded A1EPE ~{N}-[1-methyl-3-[2-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-5~{H}-pyrrolo[2,3-b]pyrazin-7-yl]indol-6-yl]propanamide × 1 SO4 SULFATE ION × 5 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.88 Å R-free 0.205
9UHC FGFR1 kinase domain with a covalent inhibitor 9p Deposited 2025-04-14 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Not recorded A1EPE ~{N}-[1-methyl-3-[2-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-5~{H}-pyrrolo[2,3-b]pyrazin-7-yl]indol-6-yl]propanamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；18% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.88 Å R-free 0.205
9UHI FGFR1 kinase domain with a covalent inhibitor 9o Deposited 2025-04-14 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Not recorded A1EPF ~{N}-[1-methyl-3-[3-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]quinoxalin-5-yl]indol-6-yl]propanamide × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；16% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.76 Å R-free 0.197
9UHI FGFR1 kinase domain with a covalent inhibitor 9o Deposited 2025-04-14 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Not recorded A1EPF ~{N}-[1-methyl-3-[3-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]quinoxalin-5-yl]indol-6-yl]propanamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277 K；16% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
Resolution 1.76 Å R-free 0.197
9VLJ Crystal structure of FGFR1 in complex with covalent inhibitor 10a Deposited 2025-06-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 458–765（308 aa）
Not recorded A1ESP ~{N}-[3-[2-[[3-[2-(dimethylamino)ethylsulfamoylmethyl]phenyl]amino]pyrimidin-4-yl]-1-methyl-indol-6-yl]propanamide × 1 SO4 SULFATE ION × 6 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 1.81 Å R-free 0.215
9VLJ Crystal structure of FGFR1 in complex with covalent inhibitor 10a Deposited 2025-06-25 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 458–765（308 aa）
Not recorded A1ESP ~{N}-[3-[2-[[3-[2-(dimethylamino)ethylsulfamoylmethyl]phenyl]amino]pyrimidin-4-yl]-1-methyl-indol-6-yl]propanamide × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
Resolution 1.81 Å R-free 0.215

77 other PDB entries and 149 assemblies. Open the comparison page and filter oligomeric states

View Construct and Data Evidence
UniProt name FGFR1_HUMAN
Isoform —
PDB entities 1
Chains and sequence ranges Author chain A； PDBConstruct 1–308； UniProt 458–765 Author chain B； PDBConstruct 1–308； UniProt 458–765

The page prioritizes protein identity, the current assembly, associated components, oligomeric state and cross-PDB links. Chain mapping and sequence ranges are retained as data evidence. Internal IDs, import timestamps and assembly operation expressions are maintenance fields and are not shown here.

SAXS scattering curve SAXS Profile

SAXS profile for 5z0s

P(r) Distance Distribution P(r) Distribution

P(r) distribution for 5z0s
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2. Structure Basics 2. Structure Basics

Entry ID entry_id5z0s
Deposition date deposition_date2017-12-20
Structure title titleCrystal structure of FGFR1 kinase domain in complex with a novel inhibitor
Keywords keywordsFGFR1 inhibitor, TRANSFERASE-TRANSFERASE INHIBITOR complex; TRANSFERASE/TRANSFERASE INHIBITOR
Experimental Method methodX-RAY DIFFRACTION
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3. SAXS Parameters (CRYSOL theoretical calculation) 3. SAXS Parameters (CRYSOL)

Radius of gyration Rg (Guinier) rg_guinier29.60 Å
Radius of gyration Rg (electron density) rg_electron28.97 Å
Forward intensity I(0) i065766100.00
Molecular weight molecular_weight64029.0 kDa
Excluded volume excluded_volume80440 ų
Envelope volume envelope_volume102830 ų
Hydration-shell volume shell_volume29905 ų
Envelope diameter envelope_diameter98.6 Å
Shell Rg shell_rg35.70 Å
Envelope Rg envelope_rg28.69 Å
Shape Rg shape_rg28.98 Å
Total Rg total_rg29.63 Å
Total atoms total_atoms4491
Residues n_residues566
Spherical-harmonic order n_harmonics20
q range q_range— – 0.5000 Å−1
Data points n_points101
Shell type shell_typedirectional
Solvent electron density solvent_density0.3340 e/ų
Shell contrast contrast_shell0.0300 e/ų
CRYSOL version crysol_version4.1.3
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4. P(r) Distance Distribution (GNOM inversion) 4. P(r) Analysis (GNOM)

Maximum dimension Dmax dmax92.5 Å
Rg (real space) rg_real29.61 Å
Rg uncertainty (real space) rg_real_error0.58 Å
I(0) (real space) i0_real6.5770e+07
I(0) uncertainty (real space) i0_real_error9.2470e+05
Rg (reciprocal space) rg_reciprocal29.61 Å
I(0) (reciprocal space) i0_reciprocal65770000.0000
Solution quality estimate total_estimate0.9023
Solution quality rating solution_quality EXCELLENT a EXCELLENT solution
P(r) peaks n_peaks2
Primary peak position r_peak_primary27.4 Å
Skewness Skewness skewness0.262
Kurtosis Kurtosis kurtosis-0.679
Angular range angular_range— – 0.2700 Å−1
Current regularization parameter α current_alpha0.0000
Highest regularization parameter α highest_alpha42180000.0000
Real-space data points n_real_points55
GNOM version gnom_version4.1.3
Quality Criteria quality_criteria AN1: 0.000; Oscil: 0.937; Stabil: 1.000; Sysdev: 1.000; Positv: 1.000; Valcen: 0.971; Smooth: 0.944
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5. Crystallography and Experiment 5. Crystallography & Experiment

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6. Entities and Polymers Entities & Polymers (3)

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7. Fold Classification (SCOP + CATH) 6 domains

SCOP 2.08 (2 domains)

Domain ID domain_idd5z0sa_
Class classd — Alpha and beta proteins (a+b)
Fold Fold foldd.144 — Protein kinase-like (PK-like)
Superfamily Superfamily superfamilyd.144.1 — Protein kinase-like (PK-like)
Family Family familyd.144.1.7 — Protein kinases, catalytic subunit
Domain ID domain_idd5z0sb_
Class classd — Alpha and beta proteins (a+b)
Fold Fold foldd.144 — Protein kinase-like (PK-like)
Superfamily Superfamily superfamilyd.144.1 — Protein kinase-like (PK-like)
Family Family familyd.144.1.7 — Protein kinases, catalytic subunit

CATH v4.4 (4 domains)

Domain ID domain_id5z0sA01
Class class3 — Alpha Beta
Architecture architecture30 — 2-Layer Sandwich
Topology topology200 — Phosphorylase Kinase; domain 1
Homologous superfamily homologous superfamily20 — Phosphorylase Kinase; domain 1
Domain ID domain_id5z0sA02
Class class1 — Mainly Alpha
Architecture architecture10 — Orthogonal Bundle
Topology topology510 — Transferase(Phosphotransferase); domain 1
Homologous superfamily homologous superfamily10 — Transferase(Phosphotransferase) domain 1
Domain ID domain_id5z0sB01
Class class3 — Alpha Beta
Architecture architecture30 — 2-Layer Sandwich
Topology topology200 — Phosphorylase Kinase; domain 1
Homologous superfamily homologous superfamily20 — Phosphorylase Kinase; domain 1
Domain ID domain_id5z0sB02
Class class1 — Mainly Alpha
Architecture architecture10 — Orthogonal Bundle
Topology topology510 — Transferase(Phosphotransferase); domain 1
Homologous superfamily homologous superfamily10 — Transferase(Phosphotransferase) domain 1
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8. Citations (1)

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9. Files and Curves (10)