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GluN2D

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Target not currently curated in GtoImmuPdb

Target id: 459

Nomenclature: GluN2D

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 1336 19q13.1 GRIN2D glutamate ionotropic receptor NMDA type subunit 2D
Mouse 3 1 1323 7 B4 Grin2d glutamate receptor, ionotropic, NMDA2D (epsilon 4)
Rat 3 1 1323 1q22 Grin2d glutamate ionotropic receptor NMDA type subunit 2D
Previous and Unofficial Names Click here for help
EB11 | NMDAR2D | GluRepsilon4 | NR2D | glutamate receptor, ionotropic, N-methyl D-aspartate 2D | glutamate receptor, ionotropic, NMDA2D (epsilon 4) | glutamate receptor
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
D-aspartic acid
D-serine
glycine
L-aspartic acid
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
glycine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
L-aspartic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glutamate site] GluN2D = GluN2B > GluN2C = GluN2A
(RS)-(tetrazol-5-yl)glycine Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
[3H]glycine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site]
D-serine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
homoquinolinic acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
[Binds to: glutamate site] GluN2B ≥ GluN2A ≥ GluN2D > GluN2C; partial agonist at GluN2A and GluN2C
NMDA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C > GluN2B > GluN2A
D-aspartic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
5,7-dichlorokynurenic acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
[Binds to: glycine site]
[3H]CGP39653 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]CGP61594 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site] [3H]CGP61594 is a photoaffinity ligand
[3H]CGS19755 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]CPP Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]L689560 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site]
[3H]MDL105519 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site]
CGP37849 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
selfotel Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
conantokin-G Peptide Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site] GluN2B > GluN2D = GluN2C = GluN2A
d-AP5 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
d-CCPene Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site] GluN2A = GluN2B > GluN2C = GluN2D
GV196771A Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
L689560 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
L701324 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
LY233053 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
UBP141 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - - 3
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [3]
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
Mg2+ Click here for species-specific activity table Hs - no - - - no
GluN2A = GluN2B > GluN2C = GluN2D
Not voltage dependent
dizocilpine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no - - - no

Not voltage dependent
[3H]dizocilpine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs - no - - - no
[Binds to: cation channel]
Not voltage dependent
amantadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no - - - no
GluN2C = GluN2D ≥ GluN2B ≥ GluN2A
Not voltage dependent
ketamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no - - - no

Not voltage dependent
N1-dansyl-spermine Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
GluN2A = GluN2B >> GluN2C = GluN2D
Not voltage dependent
phencyclidine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no - - - no

Not voltage dependent
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
DQP-1105 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Rn Negative 5.6 pIC50 - no 1
pIC50 5.6 (IC50 2.7x10-6 M) [1]
Not voltage dependent
Description: Measured using recombinant GluN1-1a NMDA subunits co-expressed with GluN2D subunits.
QNZ 46 Small molecule or natural product Primary target of this compound Rn Negative 5.4 – 5.5 pIC50 - no 2
pIC50 5.4 – 5.5 (IC50 3.9x10-6 – 3.2x10-6 M) [2]
Not voltage dependent
Description: Measured using co-expression of recombinant rGluN1 and rGluN2D. IC50 variable between expression cell lines.

References

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1. Acker TM, Yuan H, Hansen KB, Vance KM, Ogden KK, Jensen HS, Burger PB, Mullasseril P, Snyder JP, Liotta DC et al.. (2011) Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators. Mol. Pharmacol., 80 (5): 782-95. [PMID:21807990]

2. Hansen KB, Traynelis SF. (2011) Structural and mechanistic determinants of a novel site for noncompetitive inhibition of GluN2D-containing NMDA receptors. J. Neurosci., 31 (10): 3650-61. [PMID:21389220]

3. Morley RM, Tse HW, Feng B, Miller JC, Monaghan DT, Jane DE. (2005) Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists. J. Med. Chem., 48 (7): 2627-37. [PMID:15801853]

Contributors

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