当前蛋白身份：P11362
重新检索
差异标签只比较当前检索结果；所有PDB和assembly原始记录仍分别保留。
相关结构差异明细
一行代表一个 PDB 条目中的一个 biological assembly；同一蛋白的多个单体会分别列出。
| PDB 条目 | Assembly / 聚集状态 | 构建体 | 突变与修饰 | 配体、离子与非聚合物 | 实验方法 | 实验环境 | 结构质量 |
|---|---|---|---|---|---|---|---|
| 1AGW CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR 提交 1997-03-25 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
|
突变：L457V, C488A, C584S | SU2 3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
|
分辨率 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 提交 1997-03-25 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
|
突变：L457V, C488A, C584S | SU2 3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
|
分辨率 2.40 Å R-free 0.280 |
| 1CVS CRYSTAL STRUCTURE OF A DIMERIC FGF2-FGFR1 COMPLEX 提交 1999-08-24 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 4 PDB 声明：tetrameric（4） 与蛋白数一致 |
链 C
141–365（225 aa）
片段：IG-LIKE DOMAINS 2 AND 3
链 D
141–365（225 aa）
片段：IG-LIKE DOMAINS 2 AND 3
|
突变：YES 突变：YES | SO4 SULFATE ION × 4 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；ammonium sulfate, glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298K
|
分辨率 2.80 Å R-free 0.281 |
| 1CVS CRYSTAL STRUCTURE OF A DIMERIC FGF2-FGFR1 COMPLEX 提交 1999-08-24 | Assembly 2 蛋白异源复合物 异源复合物；蛋白 × 8 PDB 声明：octameric（8） 与蛋白数一致 |
链 C
141–365（225 aa）
片段：IG-LIKE DOMAINS 2 AND 3
链 D
141–365（225 aa）
片段：IG-LIKE DOMAINS 2 AND 3
|
突变：YES 突变：YES | SO4 SULFATE ION × 8 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；ammonium sulfate, glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298K
|
分辨率 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) 提交 2000-04-20 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 4 PDB 声明：tetrameric（4） 与蛋白数一致 |
链 C
141–365（225 aa）
片段：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
链 D
141–365（225 aa）
片段：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
|
未记录 | SO4 SULFATE ION × 4 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION；pH 7.5；298 K；PEG 4000, Isopropanol, HEPES-NaOH, pH 7.5, VAPOR DIFFUSION, temperature 298.0K
|
分辨率 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 提交 1997-03-22 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
|
突变：L457V, C488A, C584S | SU1 3-[(3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-YL)METHYLENE]-2-INDOLINONE × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
|
分辨率 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 提交 1997-03-22 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
|
突变：L457V, C488A, C584S | SU1 3-[(3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-YL)METHYLENE]-2-INDOLINONE × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
|
分辨率 2.50 Å R-free 0.270 |
| 1FGK CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 提交 1997-02-08 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN, HUMAN FGFR1 RESIDUES THAT POSSESS PTK ACTIVITY
链 B
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN, HUMAN FGFR1 RESIDUES THAT POSSESS PTK ACTIVITY
|
突变：L457V, C488A, C584S 突变：L457V, C488A, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5
|
分辨率 2.00 Å R-free 0.261 |
| 1FQ9 CRYSTAL STRUCTURE OF A TERNARY FGF2-FGFR1-HEPARIN COMPLEX 提交 2000-09-04 | Assembly 1 其他组合 异源复合物；蛋白 × 4 PDB 声明：tetrameric（4） 与蛋白数一致 |
链 C
141–365（225 aa）
片段：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
链 D
141–365（225 aa）
片段：EXTRACELLULAR LIGAND BINDING DOMAIN OF FGF RECEPTOR 1 (FGFR1) CONSISTING OF IMMUNOGLOBULIN LIKE DOMAINS II (D2) AND III (D3)
|
突变：N185Q 突变：N185Q | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 8.5；298 K；Ammonium sulfate, Glycerol, Tris-HCl, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
|
分辨率 3.00 Å R-free 0.282 |
| 1XR0 Structural Basis of SNT PTB Domain Interactions with Distinct Neurotrophic Receptors 提交 2004-10-13 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
409–430（22 aa）
片段：Sequence database residues 409-430 from the juxtamembrane region of hFGFR1
|
未记录 | 未记录非水小分子 | SOLUTION NMR |
NMR测量条件
pH 6.5；303 K；离子强度（mmCIF原始值）15 mM DTT-d10, and 0.5 mM EDTA00 mM phosphate buffer,；压力 1
NMR样品组成
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
|
分辨率未提供 |
| 2CR3 Solution structure of the first Ig-like domain of human fibroblast growth factor receptor 1 提交 2005-05-20 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
38–123（86 aa）
片段：Ig domain
|
未记录 | 未记录非水小分子 | SOLUTION NMR |
NMR测量条件
pH 7；298 K；离子强度（mmCIF原始值）120mM；压力 ambient
NMR样品组成
1.22mM 13C, 15N-labeled protein; 20mM d-Tris-HCl (pH7.0); 100mM NaCl; 1mM DTT; 0.02% NaN3 | 90% H2O/10% D2O
|
分辨率未提供 |
| 2FGI CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 提交 1998-09-15 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
链 B
456–765（310 aa）
片段：TYROSINE KINASE DOMAIN
|
突变：L457V, C488A, C584S 突变：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结晶条件
pH 6.5；16% PEG 10000, 0.3 M (NH4)2SO4, 100 MM BIS-TRIS, PH 6.5, 5% ETHYLENE GLYCOL
|
分辨率 2.50 Å R-free 0.264 |
| 3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole 提交 2008-01-29 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
464–765（302 aa）
片段：KINASE DOMAIN
|
突变：C488A | C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.07 Å R-free 0.264 |
| 3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole 提交 2008-01-29 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
464–765（302 aa）
片段：KINASE DOMAIN
|
突变：C488A | C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.07 Å R-free 0.264 |
| 3C4F FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole 提交 2008-01-29 | Assembly 3 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
464–765（302 aa）
片段：KINASE DOMAIN
|
突变：C488A | C4F 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine × 2 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.07 Å R-free 0.264 |
| 3DPK cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor 提交 2008-07-08 | Assembly 1 信息不足 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
577–597（21 aa）
片段：KINASE DOMAIN
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 5.2；298 K；PEG 3350, SODIUM ACETATE, LI2SO4, pH 5.2, VAPOR DIFFUSION, HANGING DROP, temperature 298K
|
分辨率 1.95 Å R-free 0.244 |
| 3GQI Crystal Structure of activated receptor tyrosine kinase in complex with substrates 提交 2009-03-24 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–774（317 aa）
片段：Protein kinase domain
|
突变：C488A, Y583F, C584S, Y575F 非标准单体：是（mmCIF未提供具体位点） | DVT DECAVANADATE × 1 ACP PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER × 1 MG MAGNESIUM ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；PEg 8000, taurine, pH 8.0, VAPOR DIFFUSION, HANGING DROP, temperature 277K
|
分辨率 2.50 Å R-free 0.289 |
| 3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates 提交 2009-03-24 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–774（317 aa）
片段：protein kinase domain
|
突变：C488A | GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
|
分辨率 2.80 Å R-free 0.289 |
| 3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates 提交 2009-03-24 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–774（317 aa）
片段：protein kinase domain
|
突变：C488A | GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
|
分辨率 2.80 Å R-free 0.289 |
| 3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates 提交 2009-03-24 | Assembly 3 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 C
458–774（317 aa）
片段：protein kinase domain
|
突变：C488A | GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
|
分辨率 2.80 Å R-free 0.289 |
| 3GQL Crystal Structure of activated receptor tyrosine kinase in complex with substrates 提交 2009-03-24 | Assembly 4 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–774（317 aa）
片段：protein kinase domain
链 B
458–774（317 aa）
片段：protein kinase domain
|
突变：C488A 突变：C488A | GQL (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol × 2 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 6.5；277 K；PEG 8000, (NH4)2SO4, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
|
分辨率 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 提交 2009-09-09 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Kinase domain: UNP residues 459-765
链 B
458–765（308 aa）
片段：Kinase domain: UNP residues 459-765
|
突变：C488A, C584S 突变：C488A, C584S | VM1 5-(2-thienyl)nicotinic acid × 2 PO4 PHOSPHATE ION × 2 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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 提交 2009-09-09 | Assembly 2 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Kinase domain: UNP residues 459-765
链 B
458–765（308 aa）
片段：Kinase domain: UNP residues 459-765
|
突变：C488A, C584S 突变：C488A, C584S | VM1 5-(2-thienyl)nicotinic acid × 2 PO4 PHOSPHATE ION × 2 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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 提交 2009-11-18 | Assembly 1 信息不足 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
577–597（21 aa）
片段：UNP residues 538-678, 753-922
|
突变：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结晶条件
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
|
分辨率 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 提交 2009-11-18 | Assembly 1 信息不足 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
577–597（21 aa）
片段：UNP residues 538-678, 753-922
|
突变：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结晶条件
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
|
分辨率 2.40 Å R-free 0.264 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 3 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 C
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 4 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 D
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 5 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
链 D
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S 突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KXX Structure of the mutant Fibroblast Growth Factor receptor 1 提交 2009-12-04 | Assembly 6 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
链 C
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, R577E, C584S 突变：C488A, R577E, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.20 Å R-free 0.263 |
| 3KY2 Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain 提交 2009-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, C584S | SO4 SULFATE ION × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.70 Å R-free 0.252 |
| 3KY2 Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain 提交 2009-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Kinase domain (UNP residues 458 to 765)
|
突变：C488A, C584S | SO4 SULFATE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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 提交 2010-08-23 | Assembly 1 其他组合 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 C
142–365（224 aa）
片段：FGFR1c
|
突变：N185Q | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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 提交 2010-08-23 | Assembly 2 蛋白异源复合物 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 D
142–365（224 aa）
片段：FGFR1c
|
突变：N185Q | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.60 Å R-free 0.309 |
| 3RHX Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 提交 2011-04-12 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
461–765（305 aa）
片段：UNP residues 461-765
|
突变：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结晶条件
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
|
分辨率 2.01 Å R-free 0.262 |
| 3RHX Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 提交 2011-04-12 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
461–765（305 aa）
片段：UNP residues 461-765
|
突变：C488A, C584S | 3RH (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine × 1 EDO 1,2-ETHANEDIOL × 4 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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) 提交 2011-09-13 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：kinase domain, UNP residues 456-769
|
突变：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结晶条件
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
|
分辨率 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) 提交 2011-09-13 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
456–765（310 aa）
片段：kinase domain, UNP residues 456-769
|
突变：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结晶条件
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
|
分辨率 2.80 Å R-free 0.261 |
| 4F63 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 1 提交 2012-05-14 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
链 B
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
|
突变：C488A, C584S 突变：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结晶条件
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
|
分辨率 2.55 Å R-free 0.287 |
| 4F64 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 6 提交 2012-05-14 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
链 B
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
|
突变：C488A, C584S 突变：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结晶条件
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
|
分辨率 2.05 Å R-free 0.269 |
| 4F65 Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8 提交 2012-05-14 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
链 B
458–765（308 aa）
片段：kinase domain (UNP residues 458-765)
|
突变：C488A, C584S 突变：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结晶条件
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
|
分辨率 2.26 Å R-free 0.235 |
| 4NK9 Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 1 提交 2013-11-12 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
链 B
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
|
突变：YES 突变：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结晶条件
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
|
分辨率 2.57 Å R-free 0.262 |
| 4NKA Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 2 提交 2013-11-12 | Assembly 1 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
链 B
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
|
突变：C488A, C584S 突变：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结晶条件
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
|
分辨率 2.19 Å R-free 0.228 |
| 4NKS Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 3 提交 2013-11-13 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
|
突变：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结晶条件
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
|
分辨率 2.50 Å R-free 0.278 |
| 4NKS Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 3 提交 2013-11-13 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN (UNP RESIDUES 458-765)
|
突变：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结晶条件
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
|
分辨率 2.50 Å R-free 0.278 |
| 4RWI Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M), apo 提交 2014-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Residues 458-765
|
突变：C488A, C584S, V561M | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.29 Å R-free 0.236 |
| 4RWI Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M), apo 提交 2014-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Residues 458-765
|
突变：C488A, C584S, V561M | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Residues 458-765
|
突变：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结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Residues 458-765
|
突变：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结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Residues 458-765
|
突变：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结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Residues 458-765
|
突变：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结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：Residues 458-765
|
突变：C488A, C584S | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 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) 提交 2014-12-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：Residues 458-765
|
突变：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结晶条件
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
|
分辨率 2.19 Å R-free 0.256 |
| 4UWB Fibroblast growth factor receptor 1 kinase in complex with JK-P5 提交 2014-08-11 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
突变：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结晶条件
20% PEG8000, 20% ETHLYENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
|
分辨率 2.31 Å R-free 0.272 |
| 4UWB Fibroblast growth factor receptor 1 kinase in complex with JK-P5 提交 2014-08-11 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
突变：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结晶条件
20% PEG8000, 20% ETHLYENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
|
分辨率 2.31 Å R-free 0.272 |
| 4UWC Fibroblast growth factor receptor 1 kinase in complex with JK-P3 提交 2014-08-11 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
突变：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结晶条件
20% PEG8000, 20% ETHYLENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
|
分辨率 1.96 Å R-free 0.206 |
| 4UWC Fibroblast growth factor receptor 1 kinase in complex with JK-P3 提交 2014-08-11 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
突变：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结晶条件
20% PEG8000, 20% ETHYLENE GLYCOL, 0.2M AMMONIUM SULPHATE, 0.1M PCTP PH 6.75
|
分辨率 1.96 Å R-free 0.206 |
| 4UWY FGFR1 Apo structure 提交 2014-08-15 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
未记录 | PEG DI(HYDROXYETHYL)ETHER × 1 CL CHLORIDE ION × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 2.31 Å R-free 0.267 |
| 4UWY FGFR1 Apo structure 提交 2014-08-15 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
未记录 | 未记录非水小分子 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 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 提交 2014-11-02 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
490–796（307 aa）
片段：UNP residues 311-490
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 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 提交 2014-11-02 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
490–796（307 aa）
片段：UNP residues 311-490
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 1.65 Å R-free 0.247 |
| 4ZSA Crystal structure of FGFR1 kinase domain in complex with 7n 提交 2015-05-13 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：UNP residues 458-765
|
突变：C488A, C584S | 4UT 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.00 Å R-free 0.254 |
| 4ZSA Crystal structure of FGFR1 kinase domain in complex with 7n 提交 2015-05-13 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：UNP residues 458-765
|
突变：C488A, C584S | 4UT 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.00 Å R-free 0.254 |
| 5A4C FGFR1 ligand complex 提交 2015-06-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
461–765（305 aa）
片段：RESIDUES 461-765
|
突变：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 未提供已读取条件 | 分辨率 2.09 Å R-free 0.235 |
| 5A4C FGFR1 ligand complex 提交 2015-06-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
461–765（305 aa）
片段：RESIDUES 461-765
|
突变：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 未提供已读取条件 | 分辨率 2.09 Å R-free 0.235 |
| 5AM6 Native FGFR1 with an inhibitor 提交 2015-03-10 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
未记录 | 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结晶条件
pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 1.96 Å R-free 0.252 |
| 5AM6 Native FGFR1 with an inhibitor 提交 2015-03-10 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, RESIDUES 458-765
|
未记录 | 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结晶条件
pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 1.96 Å R-free 0.252 |
| 5AM7 FGFR1 mutant with an inhibitor 提交 2015-03-10 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：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结晶条件
pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 1.96 Å R-free 0.254 |
| 5AM7 FGFR1 mutant with an inhibitor 提交 2015-03-10 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：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结晶条件
pH 8；20 % PEG 5K MME, 0.1 M TRIS, PH 7.5, 0.2 M (NH4)2SO4
|
分辨率 1.96 Å R-free 0.254 |
| 5B7V Human FGFR1 kinase in complex with CH5183284 提交 2016-06-09 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
456–765（310 aa）
片段：tyrosine kinase domain, UNP residues 456-765
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, (NH4)2SO4, BIS-TRIS
|
分辨率 2.15 Å R-free 0.256 |
| 5B7V Human FGFR1 kinase in complex with CH5183284 提交 2016-06-09 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
456–765（310 aa）
片段：tyrosine kinase domain, UNP residues 456-765
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 6.5；277 K；PEG 10000, (NH4)2SO4, BIS-TRIS
|
分辨率 2.15 Å R-free 0.256 |
| 5EW8 FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 提交 2015-11-20 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 6.75；277 K；18-20% PEG8000, 200mM Ammonium sulphate, 100mM PCTP, 20% (v/v) ethylene glycol
|
分辨率 1.63 Å R-free 0.206 |
| 5EW8 FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 提交 2015-11-20 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 6.75；277 K；18-20% PEG8000, 200mM Ammonium sulphate, 100mM PCTP, 20% (v/v) ethylene glycol
|
分辨率 1.63 Å R-free 0.206 |
| 5FLF DISEASE LINKED MUTATION IN FGFR 提交 2015-10-26 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：YES | SO4 SULFATE ION × 1 ACT ACETATE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
|
分辨率 2.58 Å R-free 0.255 |
| 5FLF DISEASE LINKED MUTATION IN FGFR 提交 2015-10-26 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：YES | SO4 SULFATE ION × 1 CL CHLORIDE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
|
分辨率 2.58 Å R-free 0.255 |
| 5FLF DISEASE LINKED MUTATION IN FGFR 提交 2015-10-26 | Assembly 3 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 C
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：YES | SO4 SULFATE ION × 1 CL CHLORIDE ION × 1 PGE TRIETHYLENE GLYCOL × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
|
分辨率 2.58 Å R-free 0.255 |
| 5FLF DISEASE LINKED MUTATION IN FGFR 提交 2015-10-26 | Assembly 4 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 D
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：YES | SO4 SULFATE ION × 5 CL CHLORIDE ION × 3 PGE TRIETHYLENE GLYCOL × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
|
分辨率 2.58 Å R-free 0.255 |
| 5FLF DISEASE LINKED MUTATION IN FGFR 提交 2015-10-26 | Assembly 5 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 E
458–765（308 aa）
片段：KINASE DOMAIN, UNP RESIDUES 458-765
|
突变：YES | SO4 SULFATE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
pH 7.5；20 PEG 400, 0.75 M AMMONIUM SULPHATE, 0.1 M MAGNESIUM CHLORIDE, 0.1 M HEPES PH 7.5
|
分辨率 2.58 Å R-free 0.255 |
| 5O49 Human FGF in complex with a covalent inhibitor 提交 2017-05-26 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
未记录 | 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结晶条件
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
|
分辨率 1.91 Å R-free 0.220 |
| 5O49 Human FGF in complex with a covalent inhibitor 提交 2017-05-26 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
未记录 | 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结晶条件
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
|
分辨率 1.91 Å R-free 0.220 |
| 5O4A Human FGF in complex with a covalent inhibitor 提交 2017-05-26 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 2.01 Å R-free 0.225 |
| 5O4A Human FGF in complex with a covalent inhibitor 提交 2017-05-26 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 2.01 Å R-free 0.225 |
| 5UQ0 FGFR1 kinase domain complex with fragment 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxamide 提交 2017-02-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
片段：UNP residues 457-763
|
突变：C488A, C584S | WP1 2,2-dimethyl-2,3-dihydro-1-benzofuran-7-carboxamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.30 Å R-free 0.294 |
| 5UQ0 FGFR1 kinase domain complex with fragment 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxamide 提交 2017-02-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
片段：UNP residues 457-763
|
突变：C488A, C584S | WP1 2,2-dimethyl-2,3-dihydro-1-benzofuran-7-carboxamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.30 Å R-free 0.294 |
| 5UR1 FGFR1 kinase domain complex with SN37333 in reversible binding mode 提交 2017-02-09 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.20 Å R-free 0.277 |
| 5UR1 FGFR1 kinase domain complex with SN37333 in reversible binding mode 提交 2017-02-09 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.20 Å R-free 0.277 |
| 5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 提交 2017-04-30 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
456–763（308 aa）
片段：unp residues 458-765
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
|
分辨率 2.20 Å R-free 0.223 |
| 5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 提交 2017-04-30 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
456–763（308 aa）
片段：unp residues 458-765
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
|
分辨率 2.20 Å R-free 0.223 |
| 5VND Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 提交 2017-04-30 | Assembly 3 蛋白同源多聚体 同源多聚体；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 A
456–763（308 aa）
片段：unp residues 458-765
链 B
456–763（308 aa）
片段：unp residues 458-765
|
突变：C486A, Y561C, C582S 突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；298 K；20% PEG10000, 0.1M MES pH6.2, 0.3M Ammonium Sulphate, 5% Ethylene glycol
|
分辨率 2.20 Å R-free 0.223 |
| 5W21 Crystal Structure of a 1:1:1 FGF23-FGFR1c-aKlotho Ternary Complex 提交 2017-06-05 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 3 PDB 声明：trimeric（3） 与蛋白数一致 |
链 C
142–365（224 aa）
片段：D2 and D3 region (UNP residues 142-365)
|
未记录 | NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 7 ZN ZINC ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 3.00 Å R-free 0.278 |
| 5W59 Crystal structure of a monomeric human FGF9 in complex with the ectodomain of human FGFR1c 提交 2017-06-14 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 B
142–365（224 aa）
片段：;Extracellular ligand binding domain of the "c" splice isoform (UNP residues 142-365)
;
|
未记录 | SO4 SULFATE ION × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
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
|
分辨率 2.50 Å R-free 0.221 |
| 5Z0S Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor 提交 2017-12-20 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：UNP residues 458-765
|
突变：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结晶条件
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
|
分辨率 2.45 Å R-free 0.275 |
| 5Z0S Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor 提交 2017-12-20 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：UNP residues 458-765
|
突变：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结晶条件
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
|
分辨率 2.45 Å R-free 0.275 |
| 5ZV2 FGFR-1 in complex with ligand lenvatinib 提交 2018-05-09 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
461–764（304 aa）
片段：KINASE DOMAIN
|
突变：C488A | LEV 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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.
|
分辨率 2.86 Å R-free 0.269 |
| 5ZV2 FGFR-1 in complex with ligand lenvatinib 提交 2018-05-09 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
461–764（304 aa）
片段：KINASE DOMAIN
|
突变：C488A | LEV 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
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.
|
分辨率 2.86 Å R-free 0.269 |
| 6C18 FGFR1 kinase complex with inhibitor SN37115 提交 2018-01-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.30 Å R-free 0.267 |
| 6C18 FGFR1 kinase complex with inhibitor SN37115 提交 2018-01-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.30 Å R-free 0.267 |
| 6C19 FGFR1 kinase complex with inhibitor SN36985 提交 2018-01-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.12 Å R-free 0.239 |
| 6C19 FGFR1 kinase complex with inhibitor SN36985 提交 2018-01-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.12 Å R-free 0.239 |
| 6C1B FGFR1 kinase complex with inhibitor SN37118 提交 2018-01-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.00 Å R-free 0.255 |
| 6C1B FGFR1 kinase complex with inhibitor SN37118 提交 2018-01-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.00 Å R-free 0.255 |
| 6C1C FGFR1 kinase complex with inhibitor SN37116 提交 2018-01-04 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.15 Å R-free 0.270 |
| 6C1C FGFR1 kinase complex with inhibitor SN37116 提交 2018-01-04 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
片段：UNP residues 457-763
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.15 Å R-free 0.270 |
| 6C1O FGFR1 kinase domain complexed with FIIN-1 提交 2018-01-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
457–763（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.29 Å R-free 0.276 |
| 6C1O FGFR1 kinase domain complexed with FIIN-1 提交 2018-01-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
457–763（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；20% MPEG 5000, 0.1 M sodium cacodylate pH 7.5, 0.2 M ammonium sulfate
|
分辨率 2.29 Å R-free 0.276 |
| 6ITJ Crystal structure of FGFR1 kinase domain in complex with compound 3 提交 2018-11-23 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
片段：UNP residues 458-765
|
突变：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结晶条件
VAPOR DIFFUSION；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
|
分辨率 1.99 Å R-free 0.244 |
| 6ITJ Crystal structure of FGFR1 kinase domain in complex with compound 3 提交 2018-11-23 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
片段：UNP residues 458-765
|
突变：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结晶条件
VAPOR DIFFUSION；277 K；0.1M Bis-Tris pH 6.5, 0.3M (NH4)2SO4, 15-20% PEG10000, 5% EG
|
分辨率 1.99 Å R-free 0.244 |
| 6MZQ TAS-120 in reversible binding mode with FGFR1 提交 2018-11-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
368–674（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, sodium cacodylate, ammonium sulfate
|
分辨率 2.00 Å R-free 0.230 |
| 6MZQ TAS-120 in reversible binding mode with FGFR1 提交 2018-11-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
368–674（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, sodium cacodylate, ammonium sulfate
|
分辨率 2.00 Å R-free 0.230 |
| 6MZW TAS-120 covalent complex with FGFR1 提交 2018-11-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
368–674（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, ammonium sulfate, sodium cacodylate
|
分辨率 2.20 Å R-free 0.297 |
| 6MZW TAS-120 covalent complex with FGFR1 提交 2018-11-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
368–674（307 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；291 K；MPEG 5000, ammonium sulfate, sodium cacodylate
|
分辨率 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 提交 2019-02-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 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 提交 2019-02-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 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 提交 2019-02-05 | Assembly 3 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 C
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 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 提交 2019-02-05 | Assembly 4 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 D
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.70 Å R-free 0.263 |
| 6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. 提交 2019-06-03 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.90 Å R-free 0.303 |
| 6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. 提交 2019-06-03 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.90 Å R-free 0.303 |
| 6P68 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 22. 提交 2019-06-03 | Assembly 3 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 C
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.90 Å R-free 0.303 |
| 6P69 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 11. 提交 2019-06-03 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.20 Å R-free 0.245 |
| 6P69 Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 11. 提交 2019-06-03 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
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
|
分辨率 2.20 Å R-free 0.245 |
| 7OZB FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 38. 提交 2021-06-27 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 AAA
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.71 Å R-free 0.244 |
| 7OZB FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 38. 提交 2021-06-27 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 BBB
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.71 Å R-free 0.244 |
| 7OZD FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34. 提交 2021-06-27 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 AAA
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.82 Å R-free 0.241 |
| 7OZD FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 34. 提交 2021-06-27 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 BBB
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.82 Å R-free 0.241 |
| 7OZF FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19. 提交 2021-06-28 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 AAA
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.82 Å R-free 0.242 |
| 7OZF FGFR1 kinase domain (residues 458-765) with mutations C488A, C584S in complex with 19. 提交 2021-06-28 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 BBB
458–765（308 aa）
片段：UNP residues 458-765
|
未记录 | 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结晶条件
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
|
分辨率 1.82 Å R-free 0.242 |
| 7TNH Crystal structure of CSF1R kinase domain in complex with DP-6233 提交 2022-01-21 | Assembly 1 信息不足 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
577–597（21 aa）
|
未记录 | 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结晶条件
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
|
分辨率 2.70 Å R-free 0.269 |
| 7WCL Crystal structure of FGFR1 kinase domain with Pemigatinib 提交 2021-12-20 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
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)
|
分辨率 2.50 Å R-free 0.230 |
| 7WCL Crystal structure of FGFR1 kinase domain with Pemigatinib 提交 2021-12-20 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
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)
|
分辨率 2.50 Å R-free 0.230 |
| 8JMZ FGFR1 kinase domain with sulfatinib 提交 2023-06-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：C129S | UKI Sulfatinib × 1 SO4 SULFATE ION × 6 GOL GLYCEROL × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；0.1 M MES pH 6.6,34% PEG 8000,0.2 M ammonium sulfate
|
分辨率 1.99 Å R-free 0.205 |
| 8JMZ FGFR1 kinase domain with sulfatinib 提交 2023-06-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：C129S | UKI Sulfatinib × 1 SO4 SULFATE ION × 3 GOL GLYCEROL × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；0.1 M MES pH 6.6,34% PEG 8000,0.2 M ammonium sulfate
|
分辨率 1.99 Å R-free 0.205 |
| 8JQI Cryo EM map of full length PLC gamma 2 and FGFR1 Kinase Domain 提交 2023-06-14 | Assembly 1 蛋白异源复合物 异源复合物；蛋白 × 2 PDB 声明：dimeric（2） 与蛋白数一致 |
链 B
1–822（822 aa）
|
未记录 | 未记录非水小分子 | ELECTRON MICROSCOPY |
cryo-EM缓冲液
pH 7.9；25 mM Tris pH 7.9, 150 mM NaCl, 1mM TCEP
cryo-EM玻璃化条件
冷冻剂 ETHANE
|
分辨率 4.10 Å |
| 8XLO FGFR1 kinase domain with a dual-warhead covalent inhibitor CXF-007 提交 2023-12-26 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：C584S | A1LVQ CXF007 × 1 SO4 SULFATE ION × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 2.36 Å R-free 0.255 |
| 8XLO FGFR1 kinase domain with a dual-warhead covalent inhibitor CXF-007 提交 2023-12-26 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：C584S | A1LVQ CXF007 × 1 SO4 SULFATE ION × 3 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 2.36 Å R-free 0.255 |
| 8XZ7 FGFR1 kinase domain with a covalent inhibitor 10h 提交 2024-01-20 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 1.75 Å R-free 0.225 |
| 8XZ7 FGFR1 kinase domain with a covalent inhibitor 10h 提交 2024-01-20 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 1.75 Å R-free 0.225 |
| 8Y22 FGFR1 kinase domain with a covalent inhibitor 9g 提交 2024-01-25 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 2.79 Å R-free 0.260 |
| 8Y22 FGFR1 kinase domain with a covalent inhibitor 9g 提交 2024-01-25 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 2.79 Å R-free 0.260 |
| 8YKI FGFR-1 in complex with ligand tasurgratinib 提交 2024-03-05 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
461–774（314 aa）
|
突变：C488A | A1LY1 Tasurgratinib × 1 CL CHLORIDE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；293 K；18% w/v PEG 3350, 0.2M (NH4)2 TARTRATE
|
分辨率 2.79 Å R-free 0.288 |
| 8YKI FGFR-1 in complex with ligand tasurgratinib 提交 2024-03-05 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
461–774（314 aa）
|
突变：C488A | A1LY1 Tasurgratinib × 1 CL CHLORIDE ION × 1 | X-RAY DIFFRACTION |
X-ray结晶条件
VAPOR DIFFUSION, HANGING DROP；293 K；18% w/v PEG 3350, 0.2M (NH4)2 TARTRATE
|
分辨率 2.79 Å R-free 0.288 |
| 9CD5 FGFR1 Kinase Domain Soak with Inhibitor TYRA-300 提交 2024-06-24 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；25%P8K, 25% EG, 0.25M AS, 0.1MPCTP pH7.5
|
分辨率 2.94 Å R-free 0.263 |
| 9CD5 FGFR1 Kinase Domain Soak with Inhibitor TYRA-300 提交 2024-06-24 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
突变：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结晶条件
VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；25%P8K, 25% EG, 0.25M AS, 0.1MPCTP pH7.5
|
分辨率 2.94 Å R-free 0.263 |
| 9U7G FGFR1 kinase domain with a macrocyclic compound 8g 提交 2025-03-24 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；20% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.66 Å R-free 0.216 |
| 9U7G FGFR1 kinase domain with a macrocyclic compound 8g 提交 2025-03-24 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；20% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.66 Å R-free 0.216 |
| 9UHC FGFR1 kinase domain with a covalent inhibitor 9p 提交 2025-04-14 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.88 Å R-free 0.205 |
| 9UHC FGFR1 kinase domain with a covalent inhibitor 9p 提交 2025-04-14 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；18% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.88 Å R-free 0.205 |
| 9UHI FGFR1 kinase domain with a covalent inhibitor 9o 提交 2025-04-14 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；16% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.76 Å R-free 0.197 |
| 9UHI FGFR1 kinase domain with a covalent inhibitor 9o 提交 2025-04-14 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277 K；16% (w/v) PEG 8000, 0.2 M LiSO4, and 0.1 M MES, pH 6.5
|
分辨率 1.76 Å R-free 0.197 |
| 9VLJ Crystal structure of FGFR1 in complex with covalent inhibitor 10a 提交 2025-06-25 | Assembly 1 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 A
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 1.81 Å R-free 0.215 |
| 9VLJ Crystal structure of FGFR1 in complex with covalent inhibitor 10a 提交 2025-06-25 | Assembly 2 蛋白单体 单体；蛋白 × 1 PDB 声明：monomeric（1） 与蛋白数一致 |
链 B
458–765（308 aa）
|
未记录 | 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结晶条件
VAPOR DIFFUSION, HANGING DROP；277.15 K；18% (w/v) PEG 8000, 0.2 M Li2SO4, and 0.1 M MES, pH 6.5
|
分辨率 1.81 Å R-free 0.215 |