GluK3 | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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GluK3

Target not currently curated in GtoImmuPdb

Target id: 452

Nomenclature: GluK3

Family: Ionotropic glutamate receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 919 1p34-p33 GRIK3 glutamate ionotropic receptor kainate type subunit 3
Mouse 3 1 919 4 D2.2 Grik3 glutamate receptor, ionotropic, kainate 3
Rat 3 1 919 5q36 Grik3 glutamate ionotropic receptor kainate type subunit 3
Previous and Unofficial Names
EAA5 | GluR7 | glutamate receptor 7 | GLUK7 | glutamate receptor, ionotropic, kainate 3 | glutamate receptor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Natural/Endogenous Ligands
L-glutamic acid

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
domoic acid Rn Agonist 8.4 pKi 2
pKi 8.4 (Ki 3.84x10-9 M) [2]
SYM2081 Rn Full agonist 8.2 pKi 2
pKi 8.2 (Ki 5.69x10-9 M) [2]
kainate Rn Full agonist 7.5 pKi 2
pKi 7.5 (Ki 3.28x10-8 M) low potency [2]
[3H]SYM2081 Hs Full agonist - -
[3H]kainate Hs Full agonist - -
dysiherbaine 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 Affinity Parameter Reference
[3H]UBP310 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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How to cite this page

Bernhard Bettler, Graham L. Collingridge, Ray Dingledine, Stephen F. Heinemann, Michael Hollmann, Juan Lerma, David Lodge, Mark Mayer, Masayoshi Mishina, Christophe Mulle, Shigetada Nakanishi, Richard Olsen, Stephane Peineau, John A. Peters, Peter Seeburg, Michael Spedding, Jeffrey C. Watkins.
Ionotropic glutamate receptors: GluK3. Last modified on 20/10/2015. Accessed on 23/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=452.