Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0RD7H)
Name
Glutamate receptor AMPA 3 (GRIA3)
Synonyms    Click to Show/Hide the Synonyms of This DBT
AMPA-selective glutamate receptor 3; AMPAselective glutamate receptor 3; GRIA3; GluA3; GluR-3; GluR-C; GluR-K3; GluR3; GluRC; GluRK3; Glutamate receptor ionotropic, AMPA 3
Family Transmembrane channel/porin (TC/P)  >>  Glutamate-gated ion channel (GIC)
Organism
Homo sapiens (Human)
Gene Name GRIA3 Gene ID
2892
UniProt ID GRIA3_HUMAN (click to find more protein-related data of this DBT)
TTD ID T62391 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MARQKKMGQSVLRAVFFLVLGLLGHSHGGFPNTISIGGLFMRNTVQEHSAFRFAVQLYNT
NQNTTEKPFHLNYHVDHLDSSNSFSVTNAFCSQFSRGVYAIFGFYDQMSMNTLTSFCGAL
HTSFVTPSFPTDADVQFVIQMRPALKGAILSLLGHYKWEKFVYLYDTERGFSILQAIMEA
AVQNNWQVTARSVGNIKDVQEFRRIIEEMDRRQEKRYLIDCEVERINTILEQVVILGKHS
RGYHYMLANLGFTDILLERVMHGGANITGFQIVNNENPMVQQFIQRWVRLDEREFPEAKN
APLKYTSALTHDAILVIAEAFRYLRRQRVDVSRRGSAGDCLANPAVPWSQGIDIERALKM
VQVQGMTGNIQFDTYGRRTNYTIDVYEMKVSGSRKAGYWNEYERFVPFSDQQISNDSASS
ENRTIVVTTILESPYVMYKKNHEQLEGNERYEGYCVDLAYEIAKHVRIKYKLSIVGDGKY
GARDPETKIWNGMVGELVYGRADIAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKS
KPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHLEDNNEEPRDPQSPPDPP
NEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVER
MVSPIESAEDLAKQTEIAYGTLDSGSTKEFFRRSKIAVYEKMWSYMKSAEPSVFTKTTAD
GVARVRKSKGKFAFLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGVATPKGSALRNAVNL
AVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILVGGLGLAMM
VALIEFCYKSRAESKRMKLTKNTQNFKPAPATNTQNYATYREGYNVYGTESVKI
Function
Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L- glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glutamic acid hydrochloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Acidulant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 249 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRIA3_RAT
          DIG Name: Monosodium glutamate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 3660 nM (estimated based on the structural similarity with CHEMBL575060 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRIA3_HUMAN
References
1 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators. J Med Chem. 2008 Oct 23; 51(20):6614-8.
2 Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15; 18(4):1381-7.

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