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GluK3

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Target not currently curated in GtoImmuPdb

Target id: 452

Nomenclature: GluK3

Family: Ionotropic glutamate receptors

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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
L-glutamic acid

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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

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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

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