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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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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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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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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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: | 2023-09-06 | | 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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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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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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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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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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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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3KFM
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3KEI
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3ILT
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, trichlormethiazide | | Descriptor: | 6-CHLORO-3-(DICHLOROMETHYL)-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE-7-SULFONAMIDE 1,1-DIOXIDE, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-07 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.107 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3ILU
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydroflumethiazide | | Descriptor: | 6-(trifluoromethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-07 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.003 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IL1
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, IDRA-21 | | Descriptor: | (3S)-7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-06 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.998 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IK6
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, chlorothiazide | | Descriptor: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-05 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.101 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IJX
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydrochlorothiazide | | Descriptor: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-05 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.881 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IJO
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, althiazide | | Descriptor: | (3S)-6-chloro-3-[(prop-2-en-1-ylsulfanyl)methyl]-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-04 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.003 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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2WKY
 | | Crystal structure of the ligand-binding core of GluR5 in complex with the agonist 4-AHCP | | Descriptor: | 3-(3-HYDROXY-7,8-DIHYDRO-6H-CYCLOHEPTA[D]ISOXAZOL-4-YL)-L-ALANINE, CHLORIDE ION, GLUTAMATE RECEPTOR, ... | | Authors: | Naur, P, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2009-06-18 | | Release date: | 2009-07-21 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The Glutamate Receptor Glur5 Agonist (S)-2-Amino-3-(3-Hydroxy-7,8-Dihydro-6H-Cyclohepta[D]Isoxazol-4-Yl)Propionic Acid and the 8-Methyl Analogue: Synthesis, Molecular Pharmacology, and Biostructural Characterization
J.Med.Chem., 52, 2009
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