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Title | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. |
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Journal, issue, pages | J. Med. Chem., Vol. 61, Page 251-264, Year 2018 |
Publish date | Jun 16, 2017 (structure data deposition date) |
Authors | Goffin, E. / Drapier, T. / Larsen, A.P. / Geubelle, P. / Ptak, C.P. / Laulumaa, S. / Rovinskaja, K. / Gilissen, J. / Tullio, P. / Olsen, L. ...Goffin, E. / Drapier, T. / Larsen, A.P. / Geubelle, P. / Ptak, C.P. / Laulumaa, S. / Rovinskaja, K. / Gilissen, J. / Tullio, P. / Olsen, L. / Frydenvang, K. / Pirotte, B. / Hanson, J. / Oswald, R.E. / Kastrup, J.S. / Francotte, P. |
External links | J. Med. Chem. / PubMed:29256599 |
Methods | X-ray diffraction |
Resolution | 1.78 - 2 Å |
Structure data | PDB-5o9a: PDB-5oew: |
Chemicals | ChemComp-SO4: ChemComp-7M6: ChemComp-CL: ChemComp-GOL: ChemComp-GLU: ChemComp-EDO: ChemComp-CIT: ChemComp-PEG: ChemComp-HOH: ChemComp-ZN: ChemComp-ACT: ChemComp-9TE: |
Source |
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Keywords | MEMBRANE PROTEIN / AMPA receptor / Ligand-binding domain / positive allosteric modulator / signaling protein / Ionotropic glutamate receptor / GLUA2 / GLUR2 / L504Y-N775S / Ionotropic glutamate receptor GluA2. ligand-binding domain |