Top ▲

GluK3

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 452

Nomenclature: GluK3

Family: Ionotropic glutamate receptors

Contents:

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 919 1p34.3 GRIK3 glutamate ionotropic receptor kainate type subunit 3
Mouse 3 1 919 4 58.91 cM Grik3 glutamate receptor, ionotropic, kainate 3
Rat 3 1 919 5q36 Grik3 glutamate ionotropic receptor kainate type subunit 3
Previous and Unofficial Names Click here for help
EAA5 | GluR7 | glutamate receptor 7 | GLUK7 | glutamate receptor, ionotropic, kainate 3 | glutamate receptor
Database Links Click here for help
Alphafold Q13003 (Hs), B1AS29 (Mm), P42264 (Rn)
ChEMBL Target CHEMBL3684 (Hs), CHEMBL3744 (Rn)
Ensembl Gene ENSG00000163873 (Hs), ENSMUSG00000001985 (Mm), ENSRNOG00000008992 (Rn)
Entrez Gene 2899 (Hs), 14807 (Mm), 298521 (Rn)
Human Protein Atlas ENSG00000163873 (Hs)
KEGG Gene hsa:2899 (Hs), mmu:14807 (Mm), rno:298521 (Rn)
OMIM 138243 (Hs)
Pharos Q13003 (Hs)
RefSeq Nucleotide NM_000831 (Hs), NM_001081097 (Mm), NM_001112716 (Rn)
RefSeq Protein NP_000822 (Hs), NP_001074566 (Mm), NP_001106187 (Rn)
SynPHARM 11470 (in complex with kainate)
UniProtKB Q13003 (Hs), B1AS29 (Mm), P42264 (Rn)
Wikipedia GRIK3 (Hs)
Natural/Endogenous Ligands Click here for help
L-glutamic acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
domoic acid Small molecule or natural product Ligand has a PDB structure Rn Agonist 8.4 pKi 2
⤷ pKi 8.4 (Ki 3.84x10-9 M) [2]
SYM2081 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 8.2 pKi 2
⤷ pKi 8.2 (Ki 5.69x10-9 M) [2]
kainate Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.5 pKi 2
⤷ pKi 7.5 (Ki 3.28x10-8 M) low potency [2]
[3H]SYM2081 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist - -
⤷
[3H]kainate Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist - -
⤷
dysiherbaine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
⤷
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]UBP310 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 6.3 pKd 1
⤷ pKd 6.3 (Kd 5.6x10-7 M) [1]

References

Show »

1. Atlason PT, Scholefield CL, Eaves RJ, Mayo-Martin MB, Jane DE, Molnár E. (2010) Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310. Mol Pharmacol, 78 (6): 1036-45. [PMID:20837679]

2. Sagot E, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Chapelet M, Bolte J, Gefflaut T, Bunch L. (2008) Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. J Med Chem, 51 (14): 4093-103. [PMID:18578478]

Contributors

Show »

How to cite this page