3BU3
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5HHW
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![BU of 5hhw by Molmil](/molmil-images/mine/5hhw) | Crystal structure of insulin receptor kinase domain in complex with cis-(R)-7-(3-(azetidin-1-ylmethyl)cyclobutyl)-5-(3-((tetrahydro-2H-pyran-2-yl)methoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine. | Descriptor: | 1,2-ETHANEDIOL, 7-[3-(azetidin-1-ylmethyl)cyclobutyl]-5-[3-[[(2~{R})-oxan-2-yl]methoxy]phenyl]pyrrolo[2,3-d]pyrimidin-4-amine, Insulin receptor | Authors: | Scheufler, C, Izaac, A, Stauffer, F. | Deposit date: | 2016-01-11 | Release date: | 2016-04-13 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (1.79 Å) | Cite: | Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. Bioorg.Med.Chem.Lett., 26, 2016
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5U1M
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4IBM
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![BU of 4ibm by Molmil](/molmil-images/mine/4ibm) | Crystal structure of insulin receptor kinase domain in complex with an inhibitor Irfin-1 | Descriptor: | 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-3H-pyrazolo[3,4-c]pyridazin-3-one, Insulin receptor | Authors: | Wu, J, Anastassiadis, T, Duong-Ly, K.C, Peterson, J.R. | Deposit date: | 2012-12-08 | Release date: | 2013-08-21 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor. J.Biol.Chem., 288, 2013
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1P14
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![BU of 1p14 by Molmil](/molmil-images/mine/1p14) | Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase | Descriptor: | insulin receptor | Authors: | Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R. | Deposit date: | 2003-04-11 | Release date: | 2003-07-22 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor J.Biol.Chem., 278, 2003
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1IR3
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3BU6
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1IRK
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![BU of 1irk by Molmil](/molmil-images/mine/1irk) | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HUMAN INSULIN RECEPTOR | Descriptor: | ETHYL MERCURY ION, INSULIN RECEPTOR TYROSINE KINASE DOMAIN | Authors: | Hubbard, S.R, Wei, L, Ellis, L, Hendrickson, W.A. | Deposit date: | 1995-01-02 | Release date: | 1995-02-27 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Crystal structure of the tyrosine kinase domain of the human insulin receptor. Nature, 372, 1994
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3EKK
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![BU of 3ekk by Molmil](/molmil-images/mine/3ekk) | Insulin receptor kinase complexed with an inhibitor | Descriptor: | 2-[(2-{[1-(N,N-dimethylglycyl)-5-methoxy-1H-indol-6-yl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide, Insulin receptor | Authors: | Chamberlain, S, Atkins, C, Deanda, F, Dumble, M, Gerding, R, Groy, A, Korenchuk, S, Kumar, R, Lei, H, Mook, R, Moorthy, G, Redman, A, Rowland, J, Sabbatini, P, Shewchuk, L. | Deposit date: | 2008-09-19 | Release date: | 2008-12-23 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg.Med.Chem.Lett., 19, 2009
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3BU5
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8DWN
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3EKN
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![BU of 3ekn by Molmil](/molmil-images/mine/3ekn) | Insulin receptor kinase complexed with an inhibitor | Descriptor: | 2-fluoro-6-{[2-({2-methoxy-4-[4-(1-methylethyl)piperazin-1-yl]phenyl}amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}benzamide, Insulin receptor | Authors: | Chamberlain, S, Atkins, C, Deanda, F, Dumble, M, Gerding, R, Groy, A, Korenchuk, S, Kumar, R, Lei, H, Mook, R, Moorthy, G, Redman, A, Rowland, J, Shewchuk, L. | Deposit date: | 2008-09-19 | Release date: | 2008-12-30 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett., 19, 2009
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5E1S
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![BU of 5e1s by Molmil](/molmil-images/mine/5e1s) | The Crystal structure of INSR Tyrosine Kinase in complex with the Inhibitor BI 885578 | Descriptor: | (5R)-N-(1-{2-[4-(2-methoxyethyl)piperazin-1-yl]ethyl}-1H-pyrazol-3-yl)-5,8-dimethyl-9-phenyl-6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine, Insulin receptor | Authors: | Kessler, D, Zahn, S, Sanderson, M, Wolkerstorfer, B. | Deposit date: | 2015-09-30 | Release date: | 2015-10-14 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.264 Å) | Cite: | BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis. Mol.Cancer Ther., 14, 2015
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2B4S
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![BU of 2b4s by Molmil](/molmil-images/mine/2b4s) | Crystal structure of a complex between PTP1B and the insulin receptor tyrosine kinase | Descriptor: | Insulin receptor, SULFATE ION, Tyrosine-protein phosphatase, ... | Authors: | Li, S, Depetris, R.S, Barford, D, Chernoff, J, Hubbard, S.R. | Deposit date: | 2005-09-26 | Release date: | 2005-11-15 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Crystal Structure of a Complex between Protein Tyrosine Phosphatase 1B and the Insulin Receptor Tyrosine Kinase. Structure, 13, 2005
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4XLV
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2HR7
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![BU of 2hr7 by Molmil](/molmil-images/mine/2hr7) | Insulin receptor (domains 1-3) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, ... | Authors: | Garrett, T.P.J, Ward, C.W. | Deposit date: | 2006-07-19 | Release date: | 2006-08-15 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.32 Å) | Cite: | The first three domains of the insulin receptor differ structurally from the insulin-like growth factor 1 receptor in the regions governing ligand specificity. Proc.Natl.Acad.Sci.Usa, 103, 2006
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1I44
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![BU of 1i44 by Molmil](/molmil-images/mine/1i44) | CRYSTALLOGRAPHIC STUDIES OF AN ACTIVATION LOOP MUTANT OF THE INSULIN RECEPTOR TYROSINE KINASE | Descriptor: | INSULIN RECEPTOR, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER | Authors: | Till, J.H, Ablooglu, A.J, Frankel, M, Kohanski, R.A, Hubbard, S.R. | Deposit date: | 2001-02-19 | Release date: | 2001-03-07 | Last modified: | 2023-08-09 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Crystallographic and solution studies of an activation loop mutant of the insulin receptor tyrosine kinase: insights into kinase mechanism. J.Biol.Chem., 276, 2001
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7KD6
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3ETA
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![BU of 3eta by Molmil](/molmil-images/mine/3eta) | Kinase domain of insulin receptor complexed with a pyrrolo pyridine inhibitor | Descriptor: | 1-(3-{5-[4-(aminomethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}phenyl)-3-(2-phenoxyphenyl)urea, insulin receptor, kinase domain | Authors: | Patnaik, S, Stevens, K, Gerding, R, Deanda, F, Shotwell, B, Tang, J, Hamajima, T, Nakamura, H, Leesnitzer, A, Hassell, A, Shewchuk, L, Kumar, R, Lei, H, Chamberlain, S. | Deposit date: | 2008-10-07 | Release date: | 2009-05-26 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. Bioorg.Med.Chem.Lett., 19, 2009
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1RQQ
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![BU of 1rqq by Molmil](/molmil-images/mine/1rqq) | Crystal Structure of the Insulin Receptor Kinase in Complex with the SH2 Domain of APS | Descriptor: | BISUBSTRATE INHIBITOR, Insulin receptor, MANGANESE (II) ION, ... | Authors: | Hu, J, Liu, J, Ghirlando, R, Saltiel, A.R, Hubbard, S.R. | Deposit date: | 2003-12-06 | Release date: | 2003-12-30 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structural basis for recruitment of the adaptor protein APS to the activated insulin receptor. Mol.Cell, 12, 2003
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1GAG
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![BU of 1gag by Molmil](/molmil-images/mine/1gag) | CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR | Descriptor: | BISUBSTRATE PEPTIDE INHIBITOR, INSULIN RECEPTOR, TYROSINE KINASE DOMAIN, ... | Authors: | Parang, K, Till, J.H, Ablooglu, A.J, Kohanski, R.A, Hubbard, S.R, Cole, P.A. | Deposit date: | 2000-11-29 | Release date: | 2001-01-17 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Mechanism-based design of a protein kinase inhibitor. Nat.Struct.Biol., 8, 2001
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6VEP
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![BU of 6vep by Molmil](/molmil-images/mine/6vep) | Human insulin in complex with the human insulin microreceptor in turn in complex with Fv 83-7 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, ... | Authors: | Lawrence, M.C, Menting, J.G.T. | Deposit date: | 2020-01-02 | Release date: | 2020-06-03 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | A structurally minimized yet fully active insulin based on cone-snail venom insulin principles. Nat.Struct.Mol.Biol., 27, 2020
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4XST
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![BU of 4xst by Molmil](/molmil-images/mine/4xst) | Structure of the endoglycosidase-H treated L1-CR domains of the human insulin receptor in complex with residues 697-719 of the human insulin receptor (A-isoform) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Insulin receptor, SULFATE ION, ... | Authors: | Menting, J.G, Lawrence, C.F, Kong, G.K.-W, Lawrence, M.C. | Deposit date: | 2015-01-22 | Release date: | 2015-06-10 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Structural Congruency of Ligand Binding to the Insulin and Insulin/Type 1 Insulin-like Growth Factor Hybrid Receptors. Structure, 23, 2015
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4XSS
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![BU of 4xss by Molmil](/molmil-images/mine/4xss) | Insulin-like growth factor I in complex with site 1 of a hybrid insulin receptor / Type 1 insulin-like growth factor receptor | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, Insulin receptor, ... | Authors: | Lawrence, C, Kong, G.K.-W, Menting, J.G, Lawrence, M.C. | Deposit date: | 2015-01-22 | Release date: | 2015-06-10 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Structural Congruency of Ligand Binding to the Insulin and Insulin/Type 1 Insulin-like Growth Factor Hybrid Receptors. Structure, 23, 2015
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7U6E
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![BU of 7u6e by Molmil](/molmil-images/mine/7u6e) | |