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3i81

Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with BMS-754807 [1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoro-3-pyridinyl)-2-methyl-L-prolinamide]

Method: X-RAY DIFFRACTION Dmax: 64.1 Å Quality: EXCELLENT
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1. Protein Identity and Related Structures Protein Identity & Related Structures

Insulin-like growth factor 1 receptor

Homo sapiens

UniProt P08069

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 982–1286 Fragment：Protein kinase domain, UNP residues 982-1286 EBI 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-proli namide × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed experimental conditions Resolution 2.08 Å R-free 0.265

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 3I81 Assembly / Oligomeric State Construct Mutations and Modifications Ligands, Ions and Non-polymers Method and Experimental Conditions Structure Quality
1IGR Type 1 Insulin-like growth factor receptor (DOMAINS 1-3) Deposited 1998-09-28 Different construct Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Monomer；Protein × 1 PDB declaration: monomeric
Chain A 31–492（462 aa） Fragment：UNP residues 31-492
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 2 SO4 SULFATE ION × 8 X-RAY DIFFRACTION
X-ray crystallization conditions pH 7.5；PROTEIN WAS CRYSTALLIZED FROM 2.0 M AMMONIUM SULFATE, 100 MM HEPES, PH 7.5
Resolution 2.60 Å R-free 0.304
1JQH IGF-1 receptor kinase domain Deposited 2001-08-07 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 979–1286（308 aa） Fragment：kinase domain
Mutation：E979G, Y980S MG MAGNESIUM ION × 1 SO4 SULFATE ION × 1 ANP PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；magnesium chloride, Tris, ammonium sulphate, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.10 Å R-free 0.219
1JQH IGF-1 receptor kinase domain Deposited 2001-08-07 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 979–1286（308 aa） Fragment：kinase domain
Mutation：E979G, Y980S SO4 SULFATE ION × 1 ANP PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；magnesium chloride, Tris, ammonium sulphate, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.10 Å R-free 0.219
1JQH IGF-1 receptor kinase domain Deposited 2001-08-07 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 979–1286（308 aa） Fragment：kinase domain
Mutation：E979G, Y980S SO4 SULFATE ION × 1 ANP PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；magnesium chloride, Tris, ammonium sulphate, pH 8.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.10 Å R-free 0.219
1K3A Structure of the Insulin-like Growth Factor 1 Receptor Kinase Deposited 2001-10-02 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 988–1286（299 aa） Fragment：beta chain, kinase domain (residues 988-1286)
Non-standard monomer：Yes (specific site not provided by mmCIF) ACP PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；PEG 8000, sodium chloride, HEPES, pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.10 Å R-free 0.251
1M7N Crystal Structure of Unactivated APO Insulin-like Growth Factor-1 Receptor Kinase Domain Deposited 2002-07-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 974–1294（321 aa） Fragment：kinase domain (residues 974-1286)
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 8.5；277 K；0.1M Tris-HCl, 0.2M MgCl2, 29% PEG 8000, 2% Ethylene glycol, pH 8.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 2.70 Å R-free 0.294
1M7N Crystal Structure of Unactivated APO Insulin-like Growth Factor-1 Receptor Kinase Domain Deposited 2002-07-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 974–1294（321 aa） Fragment：kinase domain (residues 974-1286)
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 8.5；277 K；0.1M Tris-HCl, 0.2M MgCl2, 29% PEG 8000, 2% Ethylene glycol, pH 8.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 2.70 Å R-free 0.294
1P4O Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. Deposited 2003-04-23 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 974–1294（321 aa） Fragment：kinase domain
Mutation：E1067A, E1069A No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 8.5；277 K；8% PEG 8k, 0.1M LiCl, 10% ethylene glycol, 10% glycerol and 0.1M Tris-HCl buffer, pH 8.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 1.50 Å R-free 0.236
1P4O Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. Deposited 2003-04-23 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 974–1294（321 aa） Fragment：kinase domain
Mutation：E1067A, E1069A No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 8.5；277 K；8% PEG 8k, 0.1M LiCl, 10% ethylene glycol, 10% glycerol and 0.1M Tris-HCl buffer, pH 8.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 1.50 Å R-free 0.236
1P4O Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. Deposited 2003-04-23 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 974–1294（321 aa） Fragment：kinase domain
Chain B 974–1294（321 aa） Fragment：kinase domain
Mutation：E1067A, E1069A Mutation：E1067A, E1069A No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP；pH 8.5；277 K；8% PEG 8k, 0.1M LiCl, 10% ethylene glycol, 10% glycerol and 0.1M Tris-HCl buffer, pH 8.5, VAPOR DIFFUSION, SITTING DROP, temperature 277K
Resolution 1.50 Å R-free 0.236
2OJ9 Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor Deposited 2007-01-12 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 982–1286（305 aa） Fragment：KINASE DOMAIN, RESIDUES 982-1286
Not recorded BMI 3-[5-(1H-IMIDAZOL-1-YL)-7-METHYL-1H-BENZIMIDAZOL-2-YL]-4-[(PYRIDIN-2-YLMETHYL)AMINO]PYRIDIN-2(1H)-ONE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions 277 K；VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.00 Å R-free 0.276
2ZM3 Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor Deposited 2008-04-10 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 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) 575 (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；0.1M Tris-HCl, pH8, 2M NaCl, 13-16% PEG6K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.257
2ZM3 Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor Deposited 2008-04-10 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 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) 575 (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；0.1M Tris-HCl, pH8, 2M NaCl, 13-16% PEG6K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.257
2ZM3 Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor Deposited 2008-04-10 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 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) 575 (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；0.1M Tris-HCl, pH8, 2M NaCl, 13-16% PEG6K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.257
2ZM3 Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor Deposited 2008-04-10 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 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) 575 (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；0.1M Tris-HCl, pH8, 2M NaCl, 13-16% PEG6K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.257
2ZM3 Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor Deposited 2008-04-10 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 5 Protein homooligomer Homooligomer；Protein × 8 PDB declaration: octameric
Chain A 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Chain B 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Chain C 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Chain D 981–1286（306 aa） Fragment：UNP residues 981-1286, IGF-1R Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) 575 (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione × 8 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8；277 K；0.1M Tris-HCl, pH8, 2M NaCl, 13-16% PEG6K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.50 Å R-free 0.257
3D94 Crystal structure of the insulin-like growth factor-1 receptor kinase in complex with PQIP Deposited 2008-05-26 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 986–1286（301 aa） Fragment：Protein Kinase domain
Non-standard monomer：Yes (specific site not provided by mmCIF) CA CALCIUM ION × 2 D94 3-[cis-3-(4-methylpiperazin-1-yl)cyclobutyl]-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-amine × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；pH 7.5；293 K；12% PEG8000, 0.1 M imidazole, pH 7.5 and 0.2 M calcium acetate, VAPOR DIFFUSION, temperature 293K
Resolution 2.30 Å R-free 0.236
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 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 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 10 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain J 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 11 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain K 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 12 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain M 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 13 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain L 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 14 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain R 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 15 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain S 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 16 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain T 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 17 Protein homooligomer Homooligomer；Protein × 8 PDB declaration: octameric
Chain C 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain D 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain G 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain H 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain K 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain L 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain M 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Chain R 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 8 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 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 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 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 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 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 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 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 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 6 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain F 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 7 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain G 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 8 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain H 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3F5P Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor Deposited 2008-11-04 Different construct Different mutation/modification Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 9 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain I 981–1286（306 aa） Fragment：IGF-1R Kinase Domain, UNP residues 981-1286
Non-standard monomer：Yes (specific site not provided by mmCIF) 741 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 8.5；277 K；0.1M Tris-HCl, pH8.5, 2M NaCl, 14% PEG6000, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.258
3LVP Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor Deposited 2010-02-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 951–1286（336 aa） Fragment：kinase domain (2P)
Not recorded PDR 3-(4-chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine × 1 EPE 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；292 K；2.4M Ammonium Sulfate, 100mM Hepes, 5% glycerol, pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 292K
Resolution 3.00 Å R-free 0.279
3LVP Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor Deposited 2010-02-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 951–1286（336 aa） Fragment：kinase domain (2P)
Not recorded PDR 3-(4-chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；292 K；2.4M Ammonium Sulfate, 100mM Hepes, 5% glycerol, pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 292K
Resolution 3.00 Å R-free 0.279
3LVP Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor Deposited 2010-02-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 951–1286（336 aa） Fragment：kinase domain (2P)
Not recorded PDR 3-(4-chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；292 K；2.4M Ammonium Sulfate, 100mM Hepes, 5% glycerol, pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 292K
Resolution 3.00 Å R-free 0.279
3LVP Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor Deposited 2010-02-22 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 951–1286（336 aa） Fragment：kinase domain (2P)
Not recorded PDR 3-(4-chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；292 K；2.4M Ammonium Sulfate, 100mM Hepes, 5% glycerol, pH 7.5, VAPOR DIFFUSION, HANGING DROP, temperature 292K
Resolution 3.00 Å R-free 0.279
3LW0 IGF-1RK in complex with ligand MSC1609119A-1 Deposited 2010-02-23 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 983–1286（304 aa） Fragment：PROTEIN KINASE, UNP residues 983-1286
Mutation：E1097A, E1099A CCX 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide × 2 X-RAY DIFFRACTION
X-ray crystallization conditions pH 0；pH 0.0
Resolution 1.79 Å R-free 0.185
3LW0 IGF-1RK in complex with ligand MSC1609119A-1 Deposited 2010-02-23 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 983–1286（304 aa） Fragment：PROTEIN KINASE, UNP residues 983-1286
Mutation：E1097A, E1099A CCX 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide × 2 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 0；pH 0.0
Resolution 1.79 Å R-free 0.185
3LW0 IGF-1RK in complex with ligand MSC1609119A-1 Deposited 2010-02-23 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 983–1286（304 aa） Fragment：PROTEIN KINASE, UNP residues 983-1286
Mutation：E1097A, E1099A CCX 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide × 2 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 0；pH 0.0
Resolution 1.79 Å R-free 0.185
3LW0 IGF-1RK in complex with ligand MSC1609119A-1 Deposited 2010-02-23 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 983–1286（304 aa） Fragment：PROTEIN KINASE, UNP residues 983-1286
Mutation：E1097A, E1099A CCX 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide × 2 X-RAY DIFFRACTION
X-ray crystallization conditions pH 0；pH 0.0
Resolution 1.79 Å R-free 0.185
3NW5 Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11B) Deposited 2010-07-09 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 982–1286（305 aa） Fragment：KINASE DOMAIN (RESIDUES 982-1286)
Not recorded LGX N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2R)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.14 Å R-free 0.254
3NW6 Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11A) Deposited 2010-07-09 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 982–1286（305 aa） Fragment：KINASE DOMAIN (RESIDUES 982-1286)
Not recorded LGW N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2S)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.253
3NW7 Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (34) Deposited 2010-07-09 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 982–1286（305 aa） Fragment：KINASE DOMAIN (RESIDUES 982-1286)
Not recorded LGV N-({4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}methyl)-6-fluoropyridine-3-carboxamide × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.11 Å R-free 0.226
3O23 Human unphosphorylated IGF1-R Kinase domain in complex with an hydantoin inhibitor Deposited 2010-07-22 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 982–1286（305 aa） Fragment：Kinase domain
Mutation：Y987F MQY (5S)-5-methyl-1-(quinolin-4-ylmethyl)-3-{4-[(trifluoromethyl)sulfonyl]phenyl}imidazolidine-2,4-dione × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.5；298 K；40% PEG400, 50mM Mes, 100mM NaCl, 10% glycerol, 5mM DTT, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.10 Å R-free 0.278
3QQU Cocrystal structure of unphosphorylated igf with pyrimidine 8 Deposited 2011-02-16 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 988–1286（299 aa） Fragment：UNP residues 988-1286
Not recorded 01P N~2~-[3-methoxy-4-(morpholin-4-yl)phenyl]-N~4~-(quinolin-3-yl)pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；0.2M Mg Acetate, 15%-17.5% PEG8K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.302
3QQU Cocrystal structure of unphosphorylated igf with pyrimidine 8 Deposited 2011-02-16 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 988–1286（299 aa） Fragment：UNP residues 988-1286
Not recorded 01P N~2~-[3-methoxy-4-(morpholin-4-yl)phenyl]-N~4~-(quinolin-3-yl)pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；0.2M Mg Acetate, 15%-17.5% PEG8K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.302
3QQU Cocrystal structure of unphosphorylated igf with pyrimidine 8 Deposited 2011-02-16 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 988–1286（299 aa） Fragment：UNP residues 988-1286
Not recorded 01P N~2~-[3-methoxy-4-(morpholin-4-yl)phenyl]-N~4~-(quinolin-3-yl)pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；0.2M Mg Acetate, 15%-17.5% PEG8K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.302
3QQU Cocrystal structure of unphosphorylated igf with pyrimidine 8 Deposited 2011-02-16 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 988–1286（299 aa） Fragment：UNP residues 988-1286
Not recorded 01P N~2~-[3-methoxy-4-(morpholin-4-yl)phenyl]-N~4~-(quinolin-3-yl)pyrimidine-2,4-diamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7.5；277 K；0.2M Mg Acetate, 15%-17.5% PEG8K, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.90 Å R-free 0.302
4D2R Human IGF in complex with a Dyrk1B inhibitor Deposited 2014-05-12 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 985–1286（302 aa） Fragment：KINASE DOMAIN, RESIDUES 985-1286
Not recorded CL CHLORIDE ION × 1 DYK N-{2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；20% PEF3350, 0.2M MGCL2, 0.1M PCTP PH 7.5
Resolution 2.10 Å R-free 0.221
5FXQ IGFR-1R complex with a pyrimidine inhibitor. Deposited 2016-03-02 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 980–1286（307 aa） Fragment：KINASE, UNP RESIDUES 980-1286
Not recorded GD5 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(5-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.30 Å R-free 0.275
5FXR IGFR-1R complex with a pyrimidine inhibitor. Deposited 2016-03-02 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 980–1286（307 aa） Fragment：KINASE, UNP RESIDUES 980-1286
Not recorded 8LN 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(3-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.40 Å R-free 0.294
5FXS IGFR-1R complex with a pyrimidine inhibitor. Deposited 2016-03-02 Different construct Different ligand/ion Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 980–1286（307 aa） Fragment：KINASE, UNP RESIDUES 980-1286
Not recorded ACT ACETATE ION × 3 OZN 2-[4-[4-[[(6Z)-5-chloranyl-6-pyrazolo[1,5-a]pyridin-3-ylidene-1H-pyrimidin-2-yl]amino]-3,5-dimethyl-pyrazol-1-yl]piperidin-1-yl]-N,N-dimethyl-ethanamide × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 1.90 Å R-free 0.214
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain A 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain B 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain C 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain D 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 5 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain E 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 6 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain F 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 7 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain G 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5HZN Structure of NVP-AEW541 in complex with IGF-1R kinase Deposited 2016-02-02 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 8 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain H 983–1286（304 aa）
Not recorded 66A 7-[cis-3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-(benzyloxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine × 1 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 6.25；293 K；25% PEG8000, 0.1M MES PH6.25, 0.2 M AMMONIUM SULFATE, 4% GLYCEROL
Resolution 2.20 Å R-free 0.218
5U8Q Structure of the ectodomain of the human Type 1 insulin-like growth factor receptor in complex with IGF-I Deposited 2016-12-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 8 PDB declaration: octameric
Chain A 31–935（905 aa）
Mutation：residues 718-741 are replaced with the sequence AGNN SO4 SULFATE ION × 4 MLT D-MALATE × 2 NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 6 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7；293 K；1.2 M ammonium sulfate, 0.1 M imidazole-malate pH 7.0. IGF-1 was included by soaking directly into the mother crystal. For full details see the primary citation.
Resolution 3.27 Å R-free 0.303
5U8R Structure of the ectodomain of the human Type 1 insulin-like growth factor receptor Deposited 2016-12-14 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 6 PDB declaration: hexameric
Chain A 31–935（905 aa）
Mutation：residues 718-741 are replaced with the sequence AGNN SO4 SULFATE ION × 2 MLT D-MALATE × 4 NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 8 IMD IMIDAZOLE × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP；pH 7；293 K；1.2 M ammonium sulfate, 0.1 M imidazole-malate pH 7.0
Resolution 3.00 Å R-free 0.285
6JK8 Cryo-EM structure of the full-length human IGF-1R in complex with insulin Deposited 2019-02-27 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 4 PDB declaration: tetrameric
Chain A 1–1367（1367 aa）
Chain B 1–1367（1367 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 6 ELECTRON MICROSCOPY
cryo-EM buffer pH 7.4；PBS with detergent
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 5.00 Å
6VWG Head region of the open conformation of the human type 1 insulin-like growth factor receptor ectodomain in complex with human insulin-like growth factor II. Deposited 2020-02-19 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Heteromer；Protein × 3 PDB declaration: trimeric
Chain A 31–935（905 aa）
Chain B 31–935（905 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 4 ELECTRON MICROSCOPY
cryo-EM buffer pH 7.5
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.21 Å
6VWH Leg region of the open conformation of the human type 1 insulin-like growth factor receptor ectodomain in complex with human insulin-like growth factor II. Deposited 2020-02-19 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 31–935（905 aa）
Chain B 31–935（905 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 7.5
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 4.26 Å
6VWI Head region of the closed conformation of the human type 1 insulin-like growth factor receptor ectodomain in complex with human insulin-like growth factor II. Deposited 2020-02-19 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Heteromer；Protein × 3 PDB declaration: trimeric
Chain A 31–935（905 aa）
Chain B 31–935（905 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 4 ELECTRON MICROSCOPY
cryo-EM buffer pH 7.5
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.70 Å
6VWJ Leg region of the closed conformation of the human type 1 insulin-like growth factor receptor ectodomain in complex with human insulin-like growth factor II Deposited 2020-02-19 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Insufficient information Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 31–935（905 aa）
Chain B 31–935（905 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 7.5
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 4.21 Å
7PH8 Structure of Insulin-like growth factor 1 receptor's transmembrane domain Deposited 2021-08-16 Different construct 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 932–962（31 aa）
Not recorded No recorded non-water small molecule SOLUTION NMR
NMR measurement conditions pH 6.7；313 K；Ionic strength (raw mmCIF value) 0.1；Pressure AMBIENT
NMR sample composition 0.5 mM [U-100% 13C; U-100% 15N] IGF1Rtm, 100 mM [U-99% 2H] DPC, 0.3 mM sodium azide, 30 mM KH2PO4, 20 mM K2HPO4, 95% H2O/5% D2O | 95% H2O/5% D2O
Resolution not provided
7S0Q Head region of a complex of IGF-I with the ectodomain of a hybrid insulin receptor / type 1 insulin-like growth factor receptor Deposited 2021-08-30 Different construct Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 3 PDB declaration: trimeric
Chain A 31–935（905 aa）
Not recorded BMA beta-D-mannopyranose × 1 NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 7 ELECTRON MICROSCOPY
cryo-EM buffer pH 8；20mM Tris pH 8.0 160mM NaCl
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.70 Å
7S8V Leg region of a complex of IGF-I with the ectodomain of a hybrid insulin receptor / type 1 insulin-like growth factor receptor Deposited 2021-09-20 Different construct Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 2 PDB declaration: dimeric
Chain A 31–935（905 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 5 ELECTRON MICROSCOPY
cryo-EM buffer pH 8
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.73 Å
7U23 Single-chain LCDV-1 viral insulin-like peptide bound to IGF-1R ectodomain, leucine-zippered form Deposited 2022-02-22 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 × 4 PDB declaration: tetrameric
Chain E 31–935（905 aa）
Chain F 31–935（905 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 8
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 4.60 Å
7V3P Cryo-EM structure of the IGF1R/insulin complex Deposited 2021-08-11 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 × 4 PDB declaration: tetrameric
Chain A 1–931（931 aa）
Chain B 1–931（931 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 4 ELECTRON MICROSCOPY
cryo-EM buffer pH 7.4
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.60 Å
7XGD Cryo-EM structure of Apo-IGF1R map 1 Deposited 2022-04-04 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 31–927（897 aa）
Chain B 31–927（897 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 4 ELECTRON MICROSCOPY
cryo-EM buffer pH 7.4
cryo-EM vitrification conditions Cryogen OTHER
Resolution 4.00 Å
7XLC conformation II of apo-IGF1R states Deposited 2022-04-21 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Protein homooligomer Homooligomer；Protein × 2 PDB declaration: dimeric
Chain A 31–927（897 aa）
Chain B 31–927（897 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 7.4
cryo-EM vitrification conditions Cryogen OTHER
Resolution 5.00 Å
7YRR Cryo-EM structure of IGF1R with two IGF1 complex Deposited 2022-08-10 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 × 4 PDB declaration: tetrameric
Chain A 31–927（897 aa）
Chain B 31–927（897 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 7.4
cryo-EM vitrification conditions Cryogen OTHER
Resolution 4.30 Å
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 2 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain BBB 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 3 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain CCC 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 4 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain DDD 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 5 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain EEE 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 6 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain FFF 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 7 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain GGG 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYI Human IGF1R with inhibitor 6 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 8 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain HHH 974–1286（313 aa）
Not recorded IER 3-[8-azanyl-1-(4-ethoxy-8-fluoranyl-2-phenyl-quinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutan-1-ol × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M Bis-Tris, 0.3 M MgCl2, 20% PEG 3350
Resolution 3.06 Å R-free 0.235
8PYJ Human IGF1R with inhibitor 8 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded IEA 5,5-dimethyl-1-(quinolin-4-ylmethyl)-3-[4-(trifluoromethylsulfonyl)phenyl]imidazolidine-2,4-dione × 1 NI NICKEL (II) ION × 1 CD CADMIUM ION × 1 ZN ZINC ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M HEPES pH 7.5-8.5, 9-12 % PEG3350, 5 mM CoCl2, 5 mM CdCl2, 5 mM MgCl2, and 5 mM NiCl2
Resolution 2.70 Å R-free 0.302
8PYK Human IGF1R with inhibitor 47 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded IC2 5,5-dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-3-[4-(trifluoromethylsulfanyl)phenyl]imidazolidine-2,4-dione × 1 NI NICKEL (II) ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M HEPES pH 7.5-8.5, 9-12 % PEG3350, 5 mM CoCl2, 5 mM CdCl2, 5 mM MgCl2, and 5 mM NiCl2
Resolution 2.23 Å R-free 0.253
8PYL Human IGF1R with inhibitor 53 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded IE0 (5S)-5-methyl-1-(1H-pyrrolo[2,3-b]pyridin-4-ylmethyl)-3-[4-(trifluoromethylsulfanyl)phenyl]imidazolidine-2,4-dione × 1 NI NICKEL (II) ION × 1 CD CADMIUM ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M HEPES pH 7.5-8.5, 9-12 % PEG3350, 5 mM CoCl2, 5 mM CdCl2, 5 mM MgCl2, and 5 mM NiCl2
Resolution 2.93 Å R-free 0.249
8PYM Human IGF1R with inhibitor 54 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded IED 5,5-dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-4-ylmethyl)-3-[4-(trifluoromethylsulfanyl)phenyl]imidazolidine-2,4-dione × 1 NI NICKEL (II) ION × 1 CD CADMIUM ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M HEPES pH 7.5-8.5, 9-12 % PEG3350, 5 mM CoCl2, 5 mM CdCl2, 5 mM MgCl2, and 5 mM NiCl2
Resolution 2.65 Å R-free 0.309
8PYN Human IGF1R with inhibitor 56 Deposited 2023-07-25 Different construct Different ligand/ion Different experimental conditions Different structure-quality metrics Assembly 1 Protein monomer Monomer；Protein × 1 PDB declaration: monomeric
Chain AAA 974–1286（313 aa）
Not recorded ICV 5,5-dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-4-ylmethyl)-3-[4-(trifluoromethylsulfonyl)phenyl]imidazolidine-2,4-dione × 1 CD CADMIUM ION × 1 NI NICKEL (II) ION × 1 ZN ZINC ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION；293 K；0.1 M HEPES pH 7.5-8.5, 9-12 % PEG3350, 5 mM CoCl2, 5 mM CdCl2, 5 mM MgCl2, and 5 mM NiCl2
Resolution 1.71 Å R-free 0.209
8TAN CryoEM structure of MFRV-VILP bound to IGF1Rzip Deposited 2023-06-27 Different construct Different mutation/modification Different oligomeric state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics Assembly 1 Other combination Heteromer；Protein × 3 PDB declaration: trimeric
Chain A 31–935（905 aa）
Chain B 31–935（905 aa）
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 11 ELECTRON MICROSCOPY
cryo-EM buffer pH 8
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.05 Å
9NCO IN-ML-15 bound to IGF1Rzip Deposited 2025-02-16 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 × 4 PDB declaration: tetrameric
Chain A 31–926（896 aa）
Chain B 31–926（896 aa）
Not recorded No recorded non-water small molecule ELECTRON MICROSCOPY
cryo-EM buffer pH 8
cryo-EM vitrification conditions Cryogen ETHANE
Resolution 3.40 Å

44 other PDB entries and 92 assemblies. Open the comparison page and filter oligomeric states

View Construct and Data Evidence
UniProt name IGF1R_HUMAN
Isoform —
PDB entities 1
Chains and sequence ranges Author chain A； PDBConstruct 3–307； UniProt 982–1286

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

SAXS scattering curve SAXS Profile

SAXS profile for 3i81

P(r) Distance Distribution P(r) Distribution

P(r) distribution for 3i81
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2. Structure Basics 2. Structure Basics

Entry ID entry_id3i81
Deposition date deposition_date2009-07-09
Structure title titleCrystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with BMS-754807 [1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoro-3-pyridinyl)-2-methyl-L-prolinamide]
Keywords keywords;HORMONE/GROWTH FACTOR, IGF-1R, KINASE DOMAIN, ATP-binding, Disease mutation, Disulfide bond, Kinase, Membrane, Nucleotide-binding, Phosphoprotein, Polymorphism, Receptor, Transferase, Transmembrane, Tyrosine-protein kinase, HORMONE ;; HORMONE
Experimental Method methodX-RAY DIFFRACTION
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3. SAXS Parameters (CRYSOL theoretical calculation) 3. SAXS Parameters (CRYSOL)

Radius of gyration Rg (Guinier) rg_guinier20.67 Å
Radius of gyration Rg (electron density) rg_electron19.65 Å
Forward intensity I(0) i019605600.00
Molecular weight molecular_weight33613.0 kDa
Excluded volume excluded_volume42055 ų
Envelope volume envelope_volume50297 ų
Hydration-shell volume shell_volume21162 ų
Envelope diameter envelope_diameter64.8 Å
Shell Rg shell_rg26.22 Å
Envelope Rg envelope_rg20.03 Å
Shape Rg shape_rg19.64 Å
Total Rg total_rg20.59 Å
Total atoms total_atoms2358
Residues n_residues296
Spherical-harmonic order n_harmonics20
q range q_range— – 0.5000 Å−1
Data points n_points101
Shell type shell_typedirectional
Solvent electron density solvent_density0.3340 e/ų
Shell contrast contrast_shell0.0300 e/ų
CRYSOL version crysol_version4.1.3
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4. P(r) Distance Distribution (GNOM inversion) 4. P(r) Analysis (GNOM)

Maximum dimension Dmax dmax64.1 Å
Rg (real space) rg_real20.58 Å
Rg uncertainty (real space) rg_real_error0.26 Å
I(0) (real space) i0_real1.9610e+07
I(0) uncertainty (real space) i0_real_error2.3560e+05
Rg (reciprocal space) rg_reciprocal20.60 Å
I(0) (reciprocal space) i0_reciprocal19610000.0000
Solution quality estimate total_estimate0.9073
Solution quality rating solution_quality EXCELLENT a EXCELLENT solution
P(r) peaks n_peaks2
Primary peak position r_peak_primary25.1 Å
Skewness Skewness skewness0.218
Kurtosis Kurtosis kurtosis-0.474
Angular range angular_range— – 0.3850 Å−1
Current regularization parameter α current_alpha0.0000
Highest regularization parameter α highest_alpha5812000.0000
Real-space data points n_real_points70
GNOM version gnom_version4.1.3
Quality Criteria quality_criteria AN1: 0.000; Oscil: 0.931; Stabil: 1.000; Sysdev: 1.000; Positv: 1.000; Valcen: 0.997; Smooth: 0.998
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5. Crystallography and Experiment 5. Crystallography & Experiment

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6. Entities and Polymers Entities & Polymers (3)

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7. Fold Classification (SCOP + CATH) 3 domains

SCOP 2.08 (1 domains)

Domain ID domain_idd3i81a_
Class classd — Alpha and beta proteins (a+b)
Fold Fold foldd.144 — Protein kinase-like (PK-like)
Superfamily Superfamily superfamilyd.144.1 — Protein kinase-like (PK-like)
Family Family familyd.144.1.7 — Protein kinases, catalytic subunit

CATH v4.4 (2 domains)

Domain ID domain_id3i81A01
Class class3 — Alpha Beta
Architecture architecture30 — 2-Layer Sandwich
Topology topology200 — Phosphorylase Kinase; domain 1
Homologous superfamily homologous superfamily20 — Phosphorylase Kinase; domain 1
Domain ID domain_id3i81A02
Class class1 — Mainly Alpha
Architecture architecture10 — Orthogonal Bundle
Topology topology510 — Transferase(Phosphotransferase); domain 1
Homologous superfamily homologous superfamily10 — Transferase(Phosphotransferase) domain 1
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8. Citations (1)

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9. Files and Curves (10)