5HE2
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![BU of 5he2 by Molmil](/molmil-images/mine/5he2) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | Descriptor: | (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.79 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE1
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![BU of 5he1 by Molmil](/molmil-images/mine/5he1) | Human GRK2 in complex with Gbetagamma subunits and CCG224062 | Descriptor: | (4~{S})-4-[4-fluoranyl-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.15 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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4BEY
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![BU of 4bey by Molmil](/molmil-images/mine/4bey) | Night blindness causing G90D rhodopsin in complex with GaCT2 peptide | Descriptor: | ACETATE ION, Guanine nucleotide-binding protein G(t) subunit alpha-1, PALMITIC ACID, ... | Authors: | Singhal, A, Ostermaier, M.K, Vishnivetskiy, S.A, Panneels, V, Homan, K.T, Tesmer, J.J.G, Veprintsev, D, Deupi, X, Gurevich, V.V, Schertler, G.F.X, Standfuss, J. | Deposit date: | 2013-03-12 | Release date: | 2013-05-08 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Insights Into Congenital Stationary Night Blindness Based on the Structure of G90D Rhodopsin. Embo Rep., 14, 2013
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5HE0
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![BU of 5he0 by Molmil](/molmil-images/mine/5he0) | Bovine GRK2 in complex with Gbetagamma subunits and CCG215022 | Descriptor: | (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE3
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![BU of 5he3 by Molmil](/molmil-images/mine/5he3) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | Descriptor: | (4~{S})-4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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6D8Z
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![BU of 6d8z by Molmil](/molmil-images/mine/6d8z) | |
5D3V
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![BU of 5d3v by Molmil](/molmil-images/mine/5d3v) | Crystal Structure of the P-Rex1 PH domain with Citrate Bound | Descriptor: | CITRATE ANION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-08-06 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.852 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5D3X
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![BU of 5d3x by Molmil](/molmil-images/mine/5d3x) | Crystal Structure of the P-Rex1 PH domain with Inositol-(1,3,4,5)-Tetrakisphosphate Bound | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-08-06 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5D3Y
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![BU of 5d3y by Molmil](/molmil-images/mine/5d3y) | Crystal Structure of the P-Rex1 PH domain with Inositol-(1,3,4,5)-Tetrakisphosphate Bound | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-08-06 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5D3W
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![BU of 5d3w by Molmil](/molmil-images/mine/5d3w) | Crystal Structure of the P-Rex1 PH domain with Sulfate Bound | Descriptor: | Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein, SULFATE ION | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-08-06 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.852 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5D27
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![BU of 5d27 by Molmil](/molmil-images/mine/5d27) | Crystal Structure of the P-Rex1 PH domain | Descriptor: | NICKEL (II) ION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-08-05 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.92 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5DO9
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![BU of 5do9 by Molmil](/molmil-images/mine/5do9) | |
5FI0
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![BU of 5fi0 by Molmil](/molmil-images/mine/5fi0) | Crystal Structure of the P-Rex1 DH/PH tandem in complex with Rac1 | Descriptor: | PHOSPHATE ION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein,Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein, Ras-related C3 botulinum toxin substrate 1 | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-12-22 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.282 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5UKM
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![BU of 5ukm by Molmil](/molmil-images/mine/5ukm) | bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as) | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cruz-Rodriguez, O, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-12 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (3.03 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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3PUH
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![BU of 3puh by Molmil](/molmil-images/mine/3puh) | |
3PUI
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![BU of 3pui by Molmil](/molmil-images/mine/3pui) | Cocaine Esterase with mutations G4C, S10C | Descriptor: | CHLORIDE ION, Cocaine esterase, SODIUM ION | Authors: | Nance, M.R, Tesmer, J.J.G. | Deposit date: | 2010-12-04 | Release date: | 2011-09-21 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.53 Å) | Cite: | Subunit stabilization and polyethylene glycolation of cocaine esterase improves in vivo residence time. Mol.Pharmacol., 80, 2011
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5UKK
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![BU of 5ukk by Molmil](/molmil-images/mine/5ukk) | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-05 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5UKL
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![BU of 5ukl by Molmil](/molmil-images/mine/5ukl) | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | Descriptor: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-05 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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3QC9
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![BU of 3qc9 by Molmil](/molmil-images/mine/3qc9) | |
6ABP
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![BU of 6abp by Molmil](/molmil-images/mine/6abp) | |
1APB
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![BU of 1apb by Molmil](/molmil-images/mine/1apb) | |
1BAP
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![BU of 1bap by Molmil](/molmil-images/mine/1bap) | |
4WBO
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![BU of 4wbo by Molmil](/molmil-images/mine/4wbo) | |
4X94
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![BU of 4x94 by Molmil](/molmil-images/mine/4x94) | |
4WNK
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![BU of 4wnk by Molmil](/molmil-images/mine/4wnk) | Crystal Structure of Bovine G Protein Coupled-Receptor Kinase 5 in Complex with CCG215022 | Descriptor: | (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, G protein-coupled receptor kinase 5, SULFATE ION | Authors: | Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2014-10-13 | Release date: | 2015-06-10 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.42 Å) | Cite: | Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor. J.Biol.Chem., 290, 2015
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