Basic fibroblast growth factor receptor 1
Homo sapiens
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 464–765 | 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 |
| 2 | Protein monomer Monomer Protein × 1 PDB declaration: monomeric（1） Consistent with protein copy count | Chain B； UniProt 464–765 | 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 |
| 3 | Protein homooligomer Homooligomer Protein × 2 PDB declaration: dimeric（2） Consistent with protein copy count | Chain A； UniProt 464–765 | 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 |
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 3C4F | 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 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 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 |
| 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 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 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 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 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 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 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 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 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 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, 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 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, 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 mutation/modification 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 mutation/modification 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 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 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 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 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 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 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：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 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：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 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 | 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 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 | 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 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 | 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 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 | 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 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：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 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：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 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：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 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：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 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：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 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：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 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：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 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：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 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）
|
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 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）
|
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 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 |
| 5Z0S Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor Deposited 2017-12-20 | 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）
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 |
| 5Z0S Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor Deposited 2017-12-20 | 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）
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 |
| 5ZV2 FGFR-1 in complex with ligand lenvatinib Deposited 2018-05-09 | Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics | Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric |
Chain A
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 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 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）
|
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 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）
|
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 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：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 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：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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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, 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 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, 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 148 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 1–302； UniProt 464–765 Author chain B； PDBConstruct 1–302； UniProt 464–765 |
