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GluK1

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Not curated in GtoImmuPdb

Target id: 450

Nomenclature: GluK1

Family: Ionotropic glutamate receptors

Annotation status:  image of a red circle Awaiting annotation  » Email us

Contents:

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 918 21q21.3 GRIK1 glutamate ionotropic receptor kainate type subunit 1
Mouse 3 1 836 16 50.23 cM Grik1 glutamate receptor, ionotropic, kainate 1
Rat 3 1 949 11q11 Grik1 glutamate ionotropic receptor kainate type subunit 1
Previous and Unofficial Names Click here for help
EAA3 | GluR5 | glutamate receptor 5 | GluK5 | Glurbeta1 | glutamate receptor
Database Links Click here for help
Alphafold P39086 (Hs), Q60934 (Mm), P22756 (Rn)
ChEMBL Target CHEMBL1918 (Hs), CHEMBL2919 (Rn)
DrugBank Target P39086 (Hs)
Ensembl Gene ENSG00000171189 (Hs), ENSMUSG00000022935 (Mm), ENSRNOG00000001575 (Rn)
Entrez Gene 2897 (Hs), 14805 (Mm), 29559 (Rn)
Human Protein Atlas ENSG00000171189 (Hs)
KEGG Gene hsa:2897 (Hs), mmu:14805 (Mm), rno:29559 (Rn)
OMIM 138245 (Hs)
Pharos P39086 (Hs)
RefSeq Nucleotide NM_175611 (Hs), NM_010348 (Mm), NM_017241 (Rn)
RefSeq Protein NP_783300 (Hs), NP_034478 (Mm), NP_058937 (Rn)
SynPHARM 11406 (in complex with dysiherbaine)
UniProtKB P39086 (Hs), Q60934 (Mm), P22756 (Rn)
Wikipedia GRIK1 (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
SYM2081 Small molecule or natural product Click here for species-specific activity table Rn Agonist 9.2 pKi 3
⤷ pKi 9.2 (Ki 6.63x10-10 M) [3]
dysiherbaine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 9.1 pKi 4
⤷ pKi 9.1 (Ki 7.4x10-10 M) [4]
SYM2081 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.5 pKi 2
⤷ pKi 8.5 (Ki 3x10-9 M) [2]
LY339434 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 7.8 – 7.9 pKi 5
⤷ pKi 7.8 – 7.9 (Ki 1.5x10-8 – 1.3x10-8 M) [5]
kainate Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pKi 5
⤷ pKi 6.8 (Ki 1.77x10-7 M) [5]
(S)-4-AHCP Small molecule or natural product Ligand has a PDB structure Hs Full agonist - -
⤷
(S)-5-iodowillardiine Small molecule or natural product Ligand has a PDB structure Hs Agonist - -
⤷
[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 - -
⤷
8-deoxy-neodysiherbaine Small molecule or natural product Hs Full agonist - -
⤷
ATPA Small molecule or natural product Hs Full agonist - -
⤷
domoic acid 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 7.7 pKd 1
⤷ pKd 7.7 (Kd 2.1x10-8 M) [1]
2,4-epi-neodysiherbaine Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷
ACET Small molecule or natural product Ligand has a PDB structure Hs Antagonist - -
⤷
LY382884 Small molecule or natural product Hs Antagonist - -
⤷
LY466195 Small molecule or natural product Hs Antagonist - -
⤷
MSVIII-19 Small molecule or natural product Hs Antagonist - -
⤷
NS3763 Small molecule or natural product Hs Antagonist - -
⤷ non-competitive
UBP302 Small molecule or natural product Ligand has a PDB structure Hs Antagonist - -
⤷
UBP310 Small molecule or natural product Ligand has a PDB structure Hs Antagonist - -
⤷
Allosteric Modulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
concanavalin A Peptide Click here for species-specific activity table Hs Positive - - - no
⤷
Not voltage dependent

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. Pedregal C, Collado I, Escribano A, Ezquerra J, Domínguez C, Mateo AI, Rubio A, Baker SR, Goldsworthy J, Kamboj RK et al.. (2000) 4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists. J Med Chem, 43 (10): 1958-68. [PMID:10821708]

3. 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]

4. Sakai R, Swanson GT, Shimamoto K, Green T, Contractor A, Ghetti A, Tamura-Horikawa Y, Oiwa C, Kamiya H. (2001) Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea. J Pharmacol Exp Ther, 296 (2): 650-8. [PMID:11160654]

5. Small B, Thomas J, Kemp M, Hoo K, Ballyk B, Deverill M, Ogden AM, Rubio A, Pedregal C, Bleakman D. (1998) LY339434, a GluR5 kainate receptor agonist. Neuropharmacology, 37 (10-11): 1261-7. [PMID:9849663]

Contributors

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Citation information

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.

Last modified on 20/10/2015.

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