5TP9
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![BU of 5tp9 by Molmil](/molmil-images/mine/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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5M2V
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![BU of 5m2v by Molmil](/molmil-images/mine/5m2v) | Structure of GluK1 ligand-binding domain (S1S2) in complex with (2S,4R)-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid at 3.18 A resolution | Descriptor: | (2~{S},4~{R})-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | Authors: | Frydenvang, K, Kastrup, J.S, Kristensen, C.M. | Deposit date: | 2016-10-13 | Release date: | 2017-01-11 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (3.18 Å) | Cite: | Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid. J. Med. Chem., 60, 2017
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5L2E
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![BU of 5l2e by Molmil](/molmil-images/mine/5l2e) | |
5L1H
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![BU of 5l1h by Molmil](/molmil-images/mine/5l1h) | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor GYKI53655 | Descriptor: | (8R)-5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-2H,7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | Deposit date: | 2016-07-29 | Release date: | 2016-10-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (3.801 Å) | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs. Neuron, 91, 2016
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5L1E
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![BU of 5l1e by Molmil](/molmil-images/mine/5l1e) | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor CP465022 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 3-(2-chlorophenyl)-2-(2-{6-[(diethylamino)methyl]pyridin-2-yl}ethyl)-6-fluoroquinazolin-4(3H)-one, Glutamate receptor 2 | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | Deposit date: | 2016-07-29 | Release date: | 2016-10-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (4.37 Å) | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs. Neuron, 91, 2016
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5L1F
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![BU of 5l1f by Molmil](/molmil-images/mine/5l1f) | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor Perampanel | Descriptor: | 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | Deposit date: | 2016-07-29 | Release date: | 2016-10-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (4 Å) | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs. Neuron, 91, 2016
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5L1G
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![BU of 5l1g by Molmil](/molmil-images/mine/5l1g) | AMPA subtype ionotropic glutamate receptor GluA2 in complex with GYKI-Br | Descriptor: | (8R)-5-(4-amino-3-bromophenyl)-N,8-dimethyl-8,9-dihydro-2H,7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | Deposit date: | 2016-07-29 | Release date: | 2016-10-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (4.507 Å) | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs. Neuron, 91, 2016
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5L1B
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![BU of 5l1b by Molmil](/molmil-images/mine/5l1b) | AMPA subtype ionotropic glutamate receptor GluA2 in Apo state | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Glutamate receptor 2 | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | Deposit date: | 2016-07-28 | Release date: | 2016-10-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (4 Å) | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs. Neuron, 91, 2016
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5KUF
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![BU of 5kuf by Molmil](/molmil-images/mine/5kuf) | GluK2EM with 2S,4R-4-methylglutamate | Descriptor: | 2S,4R-4-METHYLGLUTAMATE, Glutamate receptor ionotropic, kainate 2 | Authors: | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | Deposit date: | 2016-07-13 | Release date: | 2016-09-07 | Last modified: | 2019-11-27 | Method: | ELECTRON MICROSCOPY (3.8 Å) | Cite: | Structural basis of kainate subtype glutamate receptor desensitization. Nature, 537, 2016
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5KUH
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![BU of 5kuh by Molmil](/molmil-images/mine/5kuh) | GluK2EM with LY466195 | Descriptor: | (3S,4aR,6S,8aR)-6-{[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl}decahydroisoquinoline-3-carboxylic acid, Glutamate receptor ionotropic, kainate 2 | Authors: | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | Deposit date: | 2016-07-13 | Release date: | 2016-09-07 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (11.6 Å) | Cite: | Structural basis of kainate subtype glutamate receptor desensitization. Nature, 537, 2016
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5KK2
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![BU of 5kk2 by Molmil](/molmil-images/mine/5kk2) | Architecture of fully occupied GluA2 AMPA receptor - TARP complex elucidated by single particle cryo-electron microscopy | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | Authors: | Zhao, Y, Chen, S, Yoshioka, C, Baconguis, I, Gouaux, E. | Deposit date: | 2016-06-20 | Release date: | 2016-07-06 | Last modified: | 2018-07-18 | Method: | ELECTRON MICROSCOPY (7.3 Å) | Cite: | Architecture of fully occupied GluA2 AMPA receptor-TARP complex elucidated by cryo-EM. Nature, 536, 2016
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5KDT
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![BU of 5kdt by Molmil](/molmil-images/mine/5kdt) | Structure of the human GluN1/GluN2A LBD in complex with GNE0723 | Descriptor: | (1~{R},2~{R})-2-[7-[[5-chloranyl-3-(trifluoromethyl)pyrazol-1-yl]methyl]-5-oxidanylidene-2-(trifluoromethyl)-[1,3]thiazolo[3,2-a]pyrimidin-3-yl]cyclopropane-1-carbonitrile, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Wallweber, H.J.A, Lupardus, P.J. | Deposit date: | 2016-06-08 | Release date: | 2016-07-13 | Method: | X-RAY DIFFRACTION (2.44 Å) | Cite: | Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design. J. Med. Chem., 59, 2016
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5KCJ
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![BU of 5kcj by Molmil](/molmil-images/mine/5kcj) | Structure of the human GluN1/GluN2A LBD in complex with GNE6901 | Descriptor: | 7-[(4-fluoranylphenoxy)methyl]-3-[(1~{R},2~{R})-2-(hydroxymethyl)cyclopropyl]-2-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Wallweber, H.J.A, Lupardus, P.J. | Deposit date: | 2016-06-06 | Release date: | 2016-07-13 | Method: | X-RAY DIFFRACTION (2.09 Å) | Cite: | Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function. Neuron, 89, 2016
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5KBU
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![BU of 5kbu by Molmil](/molmil-images/mine/5kbu) | Cryo-EM structure of GluA2-2xSTZ complex at 7.8 Angstrom resolution | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2016-06-03 | Release date: | 2016-07-13 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (7.8 Å) | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy. Science, 353, 2016
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5KBS
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![BU of 5kbs by Molmil](/molmil-images/mine/5kbs) | Cryo-EM structure of GluA2-0xSTZ at 8.7 Angstrom resolution | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2016-06-03 | Release date: | 2016-07-13 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (8.7 Å) | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy. Science, 353, 2016
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5KBV
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![BU of 5kbv by Molmil](/molmil-images/mine/5kbv) | Cryo-EM structure of GluA2 bound to antagonist ZK200775 at 6.8 Angstrom resolution | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.G, Frank, J, Sobolevsky, A.I. | Deposit date: | 2016-06-03 | Release date: | 2016-07-13 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (6.8 Å) | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy. Science, 353, 2016
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5KBT
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![BU of 5kbt by Molmil](/molmil-images/mine/5kbt) | Cryo-EM structure of GluA2-1xSTZ complex at 6.4 Angstrom resolution | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2016-06-03 | Release date: | 2016-07-13 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (6.4 Å) | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy. Science, 353, 2016
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5JTY
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![BU of 5jty by Molmil](/molmil-images/mine/5jty) | Glutamate- and DCKA-bound GluN1/GluN2A agonist binding domains with MPX-007 | Descriptor: | 4-hydroxy-5,7-dimethylquinoline-2-carboxylic acid, 5-({[(3,4-difluorophenyl)sulfonyl]amino}methyl)-6-methyl-N-[(2-methyl-1,3-thiazol-5-yl)methyl]pyrazine-2-carboxamide, GLUTAMIC ACID, ... | Authors: | Mou, T.-C, Sprang, S.R, Hansen, K.B. | Deposit date: | 2016-05-10 | Release date: | 2016-09-21 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.72 Å) | Cite: | Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors. Neuron, 91, 2016
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5JEI
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![BU of 5jei by Molmil](/molmil-images/mine/5jei) | Crystal structure of the GluA2 LBD in complex with FW | Descriptor: | 1,2-ETHANEDIOL, 2-(2-METHOXYETHOXY)ETHANOL, 2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, ... | Authors: | Eibl, C, Salazar, H, Chebli, M, Plested, A.J.R. | Deposit date: | 2016-04-18 | Release date: | 2017-02-22 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (1.229 Å) | Cite: | Mechanism of partial agonism in AMPA-type glutamate receptors. Nat Commun, 8, 2017
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5IPV
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![BU of 5ipv by Molmil](/molmil-images/mine/5ipv) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 1 | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, McHaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-10 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (9.25 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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5IPU
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![BU of 5ipu by Molmil](/molmil-images/mine/5ipu) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 6 | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-09 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (15.4 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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5IPS
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![BU of 5ips by Molmil](/molmil-images/mine/5ips) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 4 | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-09 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (13.5 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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5IPT
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![BU of 5ipt by Molmil](/molmil-images/mine/5ipt) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 5 | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-09 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (14.1 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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5IOU
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![BU of 5iou by Molmil](/molmil-images/mine/5iou) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the glutamate/glycine-bound conformation | Descriptor: | GLUTAMIC ACID, GLYCINE, Ionotropic glutamate receptor subunit NR2B, ... | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-09 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (7 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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5IOV
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![BU of 5iov by Molmil](/molmil-images/mine/5iov) | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the glutamate/glycine/Ro25-6981-bound conformation | Descriptor: | 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol, GLUTAMIC ACID, GLYCINE, ... | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | Deposit date: | 2016-03-09 | Release date: | 2016-04-20 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (7.5 Å) | Cite: | Mechanism of NMDA Receptor Inhibition and Activation. Cell, 165, 2016
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