3KG2
| AMPA subtype ionotropic glutamate receptor in complex with competitive antagonist ZK 200775 | Descriptor: | Glutamate receptor 2, beta-D-mannopyranose-(1-3)-beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | Authors: | Sobolevsky, A.I, Rosconi, M.P, Gouaux, E. | Deposit date: | 2009-10-28 | Release date: | 2009-12-08 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (3.6 Å) | Cite: | X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature, 462, 2009
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3KGC
| Isolated ligand binding domain dimer of GluA2 ionotropic glutamate receptor in complex with glutamate, LY 404187 and ZK 200775 | Descriptor: | GLUTAMIC ACID, Glutamate receptor 2, N-[(2S)-2-(4'-cyanobiphenyl-4-yl)propyl]propane-2-sulfonamide, ... | Authors: | Sobolevsky, A.I, Rosconi, M.P, Gouaux, E. | Deposit date: | 2009-10-28 | Release date: | 2009-12-15 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.55 Å) | Cite: | X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor Nature, 462, 2009
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3LSF
| Piracetam bound to the ligand binding domain of GluA2 | Descriptor: | 2-(2-oxopyrrolidin-1-yl)acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | Deposit date: | 2010-02-12 | Release date: | 2010-03-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.851 Å) | Cite: | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors. J.Med.Chem., 53, 2010
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3LSL
| Piracetam bound to the ligand binding domain of GluA2 (flop form) | Descriptor: | 2-(2-oxopyrrolidin-1-yl)acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Ahmed, A.H, Oswald, R.E. | Deposit date: | 2010-02-12 | Release date: | 2010-03-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.122 Å) | Cite: | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors. J.Med.Chem., 53, 2010
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3LSW
| Aniracetam bound to the ligand binding domain of GluA3 | Descriptor: | 1-(4-METHOXYBENZOYL)-2-PYRROLIDINONE, GLUTAMIC ACID, GluA2 S1S2 domain, ... | Authors: | Ahmed, A.H, Oswald, R.E. | Deposit date: | 2010-02-13 | Release date: | 2010-03-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.752 Å) | Cite: | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors. J.Med.Chem., 53, 2010
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3LSX
| Piracetam bound to the ligand binding domain of GluA3 | Descriptor: | 2-(2-oxopyrrolidin-1-yl)acetamide, GLUTAMIC ACID, GluA3 S1S2 domain, ... | Authors: | Ahmed, A.H, Oswald, R.E. | Deposit date: | 2010-02-13 | Release date: | 2011-03-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.006 Å) | Cite: | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors. J.Med.Chem., 53, 2010
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3M3K
| Ligand binding domain (S1S2) of GluA3 (flop) | Descriptor: | GLUTAMIC ACID, Glutamate receptor 3, ZINC ION | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | Deposit date: | 2010-03-09 | Release date: | 2010-03-23 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.793 Å) | Cite: | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA. Biochemistry, 49, 2010
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3M3F
| PEPA bound to the ligand binding domain of GluA3 (flop form) | Descriptor: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 3, ... | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | Deposit date: | 2010-03-09 | Release date: | 2010-03-23 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA. Biochemistry, 49, 2010
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3M3L
| PEPA bound to the ligand binding domain of GluA2 (flop form) | Descriptor: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | Deposit date: | 2010-03-09 | Release date: | 2010-03-23 | Last modified: | 2024-10-09 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA. Biochemistry, 49, 2010
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2XHD
| Crystal structure of N-((2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H- inden-2-yl)-2-propanesulfonamide in complex with the ligand binding domain of the human GluA2 receptor | Descriptor: | GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, N-[(2S)-5-(6-FLUORO-3-PYRIDINYL)-2,3-DIHYDRO-1H-INDEN-2-YL]-2-PROPANESULFONAMIDE, ... | Authors: | Ward, S.E, Harries, M, Aldegheri, L, Andreotti, D, Ballantine, S, Bax, B.D, Harris, A.J, Harker, A.J, Lund, J, Melarange, R, Mingardi, A, Mookherjee, C, Mosley, J, Neve, M, Oliosi, B, Profeta, R, Smith, K.J, Smith, P.W, Spada, S, Thewlis, K.M, Yusaf, S.P. | Deposit date: | 2010-06-14 | Release date: | 2010-07-21 | Last modified: | 2011-07-13 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Discovery of N-[(2S)-5-(6-Fluoro-3-Pyridinyl)-2,3-Dihydro-1H-Inden-2-Yl]-2-Propanesulfonamide, a Novel Clinical Ampa Receptor Positive Modulator. J.Med.Chem., 53, 2010
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3O2A
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ... | Authors: | Maclean, J.K.F, Basten, S, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Papakosta, M, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-22 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies. Bioorg.Med.Chem.Lett., 20, 2010
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3O29
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ... | Authors: | Maclean, J.K.F, Basten, S, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Papakosta, M, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-22 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (2.02 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies. Bioorg.Med.Chem.Lett., 20, 2010
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3O28
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | 2-({[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetyl}amino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, DIMETHYL SULFOXIDE, GLUTAMIC ACID, ... | Authors: | Maclean, J.K.F, Basten, S, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Papakosta, M, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-22 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies. Bioorg.Med.Chem.Lett., 20, 2010
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3O6I
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | 2-[({3-tert-butyl-4-[(methylamino)methyl]-1H-pyrazol-1-yl}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-29 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization. Bioorg.Med.Chem.Lett., 20, 2010
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3O6H
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | 1,2-ETHANEDIOL, 2-[({4-[(ethylamino)methyl]-3-(trifluoromethyl)-1H-pyrazol-1-yl}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, DIMETHYL SULFOXIDE, ... | Authors: | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-29 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization. Bioorg.Med.Chem.Lett., 20, 2010
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3O6G
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | 1,2-ETHANEDIOL, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | Deposit date: | 2010-07-29 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization. Bioorg.Med.Chem.Lett., 20, 2010
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3OEM
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3OEL
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3OEK
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3OEN
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3PD8
| X-ray structure of the ligand-binding core of GluA2 in complex with (S)-7-HPCA at 2.5 A resolution | Descriptor: | (7S)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-7-carboxylic acid, ACETIC ACID, CACODYLATE ION, ... | Authors: | Frydenvang, K, Kastrup, J.S. | Deposit date: | 2010-10-22 | Release date: | 2010-12-29 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.476 Å) | Cite: | Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid. J. Med. Chem., 53, 2010
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3PD9
| X-ray structure of the ligand-binding core of GluA2 in complex with (R)-5-HPCA at 2.1 A resolution | Descriptor: | (5R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid, CHLORIDE ION, GLYCEROL, ... | Authors: | Frydenvang, K, Kastrup, J.S. | Deposit date: | 2010-10-22 | Release date: | 2010-12-29 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid. J. Med. Chem., 53, 2010
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2XX7
| Crystal structure of 1-(4-(1-pyrrolidinylcarbonyl)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 2.2A resolution. | Descriptor: | 1-[4-(1-PYRROLIDINYLCARBONYL)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: | 2010-11-09 | Release date: | 2011-04-06 | Last modified: | 2011-09-28 | Method: | X-RAY DIFFRACTION (2.2 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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2XX9
| Crystal structure of 1-((2-fluoro-4-(3-(trifluoromethyl)-4,5,6,7- tetrahydro-1H-indazol-1-yl)phenyl)methyl)-2-pyrrolidinone 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: | 2011-04-06 | Last modified: | 2024-10-16 | Method: | X-RAY DIFFRACTION (1.97 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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