Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

Gria3 (P19492) - Overview - Molecular Target Synopsis

Protein


Gria3, Glutamate receptor 3
UniProt P19492

Also Known as GRIA3_RAT, Gria3, Glur3

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. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate. Homotetramer or heterotetramer of pore-forming glutamate receptor subunits. Tetramers may be formed by the dimerization of dimers. Interacts with PRKCABP, GRIP1 and GRIP2. Found in a complex with GRIA1, GRIA2, GRIA4, CNIH2, CNIH3, CACNG2, CACNG3, CACNG4, CACNG5, CACNG7 and CACNG8. Interacts with CACNG5.

6NJN
STRUCTURE OF A COMPLEX
RCSB/PDB
Inspect Structure
See all 3D Structures for Gria3

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
888P19492-2
888P19492-1

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project Gria3 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For Gria3 there are:
26 structures (43 chains) solved
23 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

Gria3 is solved in complex with the approved drug(s):

PZI/PIRACETAM (3LSX_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Gria3 has been screened with 1422 compounds (2283 bioactivities), 322 compounds have bioactivities that show binding affinity of <= 500nM (456 bioactivities). (see details)