2XXH
 
 | | Crystal structure of 1-(4-(2-oxo-2-(1-pyrrolidinyl)ethyl)phenyl)-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazole in complex with the ligand binding domain of the Rat GluA2 receptor and glutamate at 1.5A resolution. | | Descriptor: | 1-{4-[2-OXO-2-(1-PYRROLIDINYL)ETHYL]PHENYL}-3-( TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE, GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, ... | | Authors: | Ward, S.E, Harries, M, Aldegheri, L, Austin, N.E, Ballantine, S, Ballini, E, Bradley, D.M, Bax, B.D, Clarke, B.P, Harris, A.J, Harrison, S.A, Melarange, R.A, Mookherjee, C, Mosley, J, DalNegro, G, Oliosi, B, Smith, K.J, Thewlis, K.M, Woollard, P.M, Yusaf, S.P. | | Deposit date: | 2010-11-10 | | Release date: | 2011-04-06 | | Last modified: | 2011-09-28 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of Ampa Receptor Positive Allosteric Modulators.
J.Med.Chem., 54, 2011
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2XX8
 | | Crystal structure of N,N-dimethyl-4-(3-(trifluoromethyl)-4,5,6,7- tetrahydro-1H-indazol-1-yl)benzamide in complex with the ligand binding domain of the Rat GluA2 receptor and glutamate at 2.2A resolution. | | Descriptor: | GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, N,N-DIMETHYL-4-[3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOL-1-YL]BENZAMIDE, ... | | Authors: | Ward, S.E, Harries, M, Aldegheri, L, Austin, N.E, Ballantine, S, Ballini, E, Bradley, D.M, Bax, B.D, Clarke, B.P, Harris, A.J, Harrison, S.A, Melarange, R.A, Mookherjee, C, Mosley, J, DalNegro, G, Oliosi, B, Smith, K.J, Thewlis, K.M, Woollard, P.M, Yusaf, S.P. | | Deposit date: | 2010-11-09 | | Release date: | 2011-04-27 | | Last modified: | 2011-09-28 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of Ampa Receptor Positive Allosteric Modulators.
J.Med.Chem., 54, 2011
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2XXX
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2XXT
 | | Crystal structure of the GluK2 (GluR6) wild-type LBD dimer in complex with kainate | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, CHLORIDE ION, GLUTAMATE RECEPTOR, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2010-11-12 | | Release date: | 2011-02-09 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Conformational Flexibility of the Ligand-Binding Domain Dimer in Kainate Receptor Gating and Desensitization
J.Neurosci., 31, 2011
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2XXR
 | | Crystal structure of the GluK2 (GluR6) wild-type LBD dimer in complex with glutamate | | Descriptor: | CHLORIDE ION, GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2010-11-11 | | Release date: | 2011-02-09 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Conformational Flexibility of the Ligand-Binding Domain Dimer in Kainate Receptor Gating and Desensitization
J.Neurosci., 31, 2011
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2XXU
 | | Crystal structure of the GluK2 (GluR6) M770K LBD dimer in complex with glutamate | | Descriptor: | CHLORIDE ION, GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2010-11-12 | | Release date: | 2011-02-09 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Conformational Flexibility of the Ligand-Binding Domain Dimer in Kainate Receptor Gating and Desensitization
J.Neurosci., 31, 2011
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2XXW
 | | Crystal structure of the GluK2 (GluR6) D776K LBD dimer in complex with glutamate | | Descriptor: | CHLORIDE ION, GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2010-11-12 | | Release date: | 2011-02-09 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Conformational Flexibility of the Ligand-Binding Domain Dimer in Kainate Receptor Gating and Desensitization
J.Neurosci., 31, 2011
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2XXY
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2XXV
 | | Crystal structure of the GluK2 (GluR6) M770K LBD dimer in complex with kainate | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, CHLORIDE ION, GLUTAMATE RECEPTOR, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2010-11-12 | | Release date: | 2011-02-09 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Conformational Flexibility of the Ligand-Binding Domain Dimer in Kainate Receptor Gating and Desensitization
J.Neurosci., 31, 2011
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2ZNS
 | | Crystal structure of the ligand-binding core of the human ionotropic glutamate receptor, GluR5, in complex with glutamate | | Descriptor: | GLUTAMIC ACID, Glutamate receptor, ionotropic kainate 1 | | Authors: | Unno, M, Sasaki, M, Ikeda-Saito, M. | | Deposit date: | 2008-05-01 | | Release date: | 2009-05-05 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Binding and Selectivity of the Marine Toxin Neodysiherbaine A and Its Synthetic Analogues to GluK1 and GluK2 Kainate Receptors.
J.Mol.Biol., 413, 2011
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2ZNU
 | | Crystal structure of the ligand-binding core of the human ionotropic glutamate receptor, GluR5, in complex with a novel selective agonist, neodysiherbaine A | | Descriptor: | (2R,3aR,6R,7R,7aR)-2-[(2S)-2-amino-2-carboxyethyl]-6,7-dihydroxyhexahydro-2H-furo[3,2-b]pyran-2-carboxylic acid, BETA-MERCAPTOETHANOL, Glutamate receptor, ... | | Authors: | Unno, M, Sasaki, M, Ikeda-Saito, M. | | Deposit date: | 2008-05-01 | | Release date: | 2009-05-05 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Binding and Selectivity of the Marine Toxin Neodysiherbaine A and Its Synthetic Analogues to GluK1 and GluK2 Kainate Receptors.
J.Mol.Biol., 413, 2011
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2ZNT
 | | Crystal structure of the ligand-binding core of the human ionotropic glutamate receptor, GluR5, in complex with a novel selective agonist, dysiherbaine | | Descriptor: | (2R,3aR,6S,7R,7aR)-2-[(2S)-2-amino-2-carboxyethyl]-6-hydroxy-7-(methylamino)hexahydro-2H-furo[3,2-b]pyran-2-carboxylic acid, BETA-MERCAPTOETHANOL, Glutamate receptor, ... | | Authors: | Unno, M, Sasaki, M, Ikeda-Saito, M. | | Deposit date: | 2008-05-01 | | Release date: | 2009-05-05 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Binding and Selectivity of the Marine Toxin Neodysiherbaine A and Its Synthetic Analogues to GluK1 and GluK2 Kainate Receptors.
J.Mol.Biol., 413, 2011
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3BFT
 | | Structure of the ligand-binding core of GluR2 in complex with the agonist (S)-TDPA at 2.25 A resolution | | Descriptor: | (2S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propanoic acid, CACODYLATE ION, CHLORIDE ION, ... | | Authors: | Beich-Frandsen, M, Mirza, O, Vestergaard, B, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2007-11-23 | | Release date: | 2008-10-28 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.27 Å) | | Cite: | Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
J.Med.Chem., 51, 2008
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3B6T
 | | Crystal Structure of the GLUR2 Ligand Binding Core (S1S2J) T686A Mutant in Complex with Quisqualate at 2.1 Resolution | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, Glutamate receptor 2, SULFATE ION | | Authors: | Cho, Y, Lolis, E, Howe, J.R. | | Deposit date: | 2007-10-29 | | Release date: | 2008-02-05 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural and single-channel results indicate that the rates of ligand binding domain closing and opening directly impact AMPA receptor gating.
J.Neurosci., 28, 2008
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3B7D
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3BBR
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3B6Q
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3B6W
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3BFU
 | | Structure of the ligand-binding core of GluR2 in complex with the agonist (R)-TDPA at 1.95 A resolution | | Descriptor: | (2R)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propanoic acid, Glutamate receptor 2 | | Authors: | Beich-Frandsen, M, Mirza, O, Vestergaard, B, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2007-11-23 | | Release date: | 2008-10-14 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
J.Med.Chem., 51, 2008
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3C33
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5U8C
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3C36
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3C34
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5TP9
 | | Structure of the human GluN1/GluN2A LBD in complex with compound 2 (GNE9178) | | Descriptor: | 7-{[5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl}-N-ethyl-2-methyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide, ACETATE ION, CALCIUM ION, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2016-10-20 | | Release date: | 2016-11-30 | | Last modified: | 2017-02-08 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.
ACS Med Chem Lett, 8, 2017
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3C35
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