Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T42392 | Target Info | |||
| Target Name | Glutamate receptor AMPA 2 (GRIA2) | ||||
| Synonyms | Glutamate receptor ionotropic, AMPA 2; Glutamate receptor 2; GluRK2; GluRB; GluR2; GluR-K2; GluR-B; GluR-2; GluA2; AMPAselective glutamate receptor 2; AMPA-selective glutamate receptor 2 | ||||
| Target Type | Successful Target | ||||
| Gene Name | GRIA2 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | 9-(4-Tert-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide | Ligand Info | |||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)C2=CC=CN3C2=NS(=O)(=O)CC3 | ||||
| InChI | 1S/C17H20N2O2S/c1-17(2,3)14-8-6-13(7-9-14)15-5-4-10-19-11-12-22(20,21)18-16(15)19/h4-10H,11-12H2,1-3H3 | ||||
| InChIKey | NFUZLMGYOAJDAK-UHFFFAOYSA-N | ||||
| PubChem Compound ID | 66748417 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 5ZG2 Crystal structure of the GluA2o LBD in complex with ZK200775 and Compound-2 | ||||||
| Method | X-ray diffraction | Resolution | 1.25 Å | Mutation | No | [1] |
| PDB Sequence |
KTVVVTTILE
423 SPYVMMKKNH433 EMLEGNERYE443 GYCVDLAAEI453 AKHCGFKYKL463 TIVGDGKYGA 473 RDADTKIWNG483 MVGELVYGKA493 DIAIAPLTIT503 LVREEVIDFS513 KPFMSLGISI 523 MIKKGTPIES656 AEDLSKQTEI666 AYGTLDSGST676 KEFFRRSKIA686 VFDKMWTYMR 696 SAEPSVFVRT706 TAEGVARVRK716 SKGKYAYLLE726 STMNEYIEQR736 KPCDTMKVGG 746 NLDSKGYGIA756 TPKGSSLRNA766 VNLAVLKLNE776 QGLLDKLKNK786 WWYDKGECG |
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| PDB ID: 5ZG1 Crystal structure of the GluA2o LBD in complex with glutamate and Compound-2 | ||||||
| Method | X-ray diffraction | Resolution | 1.32 Å | Mutation | No | [1] |
| PDB Sequence |
KTVVVTTILE
423 SPYVMMKKNH433 EMLEGNERYE443 GYCVDLAAEI453 AKHCGFKYKL463 TIVGDGKYGA 473 RDADTKIWNG483 MVGELVYGKA493 DIAIAPLTIT503 LVREEVIDFS513 KPFMSLGISI 523 MIKKGTPIES656 AEDLSKQTEI666 AYGTLDSGST676 KEFFRRSKIA686 VFDKMWTYMR 696 SAEPSVFVRT706 TAEGVARVRK716 SKGKYAYLLE726 STMNEYIEQR736 KPCDTMKVGG 746 NLDSKGYGIA756 TPKGSSLRNA766 VNLAVLKLNE776 QGLLDKLKNK786 WWYDKGEC |
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window. Neuropsychopharmacology. 2019 Apr;44(5):961-970. | ||||
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