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GluN2C

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Not curated in GtoImmuPdb

Target id: 458

Nomenclature: GluN2C

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 1233 17q25.1 GRIN2C glutamate ionotropic receptor NMDA type subunit 2C
Mouse 3 1 1239 11 80.8 cM Grin2c glutamate receptor, ionotropic, NMDA2C (epsilon 3)
Rat 3 1 1237 10q32.1 Grin2c glutamate ionotropic receptor NMDA type subunit 2C
Previous and Unofficial Names Click here for help
NMDAR2C | glutamate [NMDA] receptor subunit epsilon-3 | GluRepsilon3 | glutamate receptor, ionotropic, NMDA2C (epsilon 3) | glutamate receptor
Database Links Click here for help
Alphafold Q14957 (Hs), Q01098 (Mm), Q00961 (Rn)
ChEMBL Target CHEMBL4109 (Hs), CHEMBL3832634 (Mm), CHEMBL401 (Rn)
DrugBank Target Q14957 (Hs), Q14957 (Hs)
Ensembl Gene ENSG00000161509 (Hs), ENSMUSG00000020734 (Mm), ENSRNOG00000003280 (Rn)
Entrez Gene 2905 (Hs), 14813 (Mm), 24411 (Rn)
Human Protein Atlas ENSG00000161509 (Hs)
KEGG Gene hsa:2905 (Hs), mmu:14813 (Mm), rno:24411 (Rn)
OMIM 138254 (Hs)
Pharos Q14957 (Hs)
RefSeq Nucleotide NM_000835 (Hs), NM_010350 (Mm), NM_012575 (Rn)
RefSeq Protein NP_000826 (Hs), NP_034480 (Mm), NP_036707 (Rn)
UniProtKB Q14957 (Hs), Q01098 (Mm), Q00961 (Rn)
Wikipedia GRIN2C (Hs)
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
memantine Small molecule or natural product Approved drug Rn Antagonist 6.2 pKi 4
⤷ pKi 6.2 (Ki 7x10-7 M) [4]
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]
View species-specific antagonist tables
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
phencyclidine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no 7.1 pIC50 - no 2
⤷ pIC50 7.1 (IC50 7.7x10-8 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
dextrorphan Small molecule or natural product Hs - no 6.9 pIC50 - no 2
⤷ pIC50 6.9 (IC50 1.14x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
dextromethorphan Small molecule or natural product Approved drug Click here for species-specific activity table Hs - no 6.3 pIC50 - no 2
⤷ pIC50 6.3 (IC50 4.66x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
levorphanol Small molecule or natural product Approved drug Click here for species-specific activity table Hs - no 6.2 pIC50 - no 2
⤷ pIC50 6.2 (IC50 6.01x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
ketamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no 6.2 pIC50 - no 2
⤷ pIC50 6.2 (IC50 6.6x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
amantadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no 4.7 pIC50 - no 2
⤷ pIC50 4.7 (IC50 2.25x10-5 M) GluN2C = GluN2D ≥ GluN2B ≥ GluN2A [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
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
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
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 8.1 pIC50 - no 1
⤷ pIC50 8.1 (IC50 7x10-9 M) [1]
Not voltage dependent
Description: Measured using recombinant GluN1-1a NMDA subunits co-expressed with GluN2C subunits.

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. Dravid SM, Erreger K, Yuan H, Nicholson K, Le P, Lyuboslavsky P, Almonte A, Murray E, Mosely C, Barber J et al.. (2007) Subunit-specific mechanisms and proton sensitivity of NMDA receptor channel block. J Physiol (Lond.), 581 (Pt 1): 107-28. [PMID:17303642]

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]

4. Williams M, Kowaluk EA, Arneric SP. (1999) Emerging molecular approaches to pain therapy. J Med Chem, 42 (9): 1481-500. [PMID:10229619]

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 21/10/2020.

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