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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1972
Target Type SINGLE PROTEIN
Preferred Name Glutamate [NMDA] receptor subunit epsilon 1
Synonyms GRIN2A | GluN2A | Glutamate [NMDA] receptor subunit epsilon-1 | Glutamate receptor ionotropic, NMDA 2A | N-methyl D-aspartate receptor subtype 2A | NMDAR2A | NMDAR2A | NR2A | hNR2A
Organism Homo sapiens
Species Group No
Protein Target Classification
  • ion channel > ligand-gated ion channel > ionotropic glutamate receptor > nmda receptor

Target Components

Component Description Relationship Accession
Glutamate receptor ionotropic, NMDA 2A SINGLE PROTEIN Q12879

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2094124 Glutamate [NMDA] receptor PROTEIN COMPLEX GROUP
CHEMBL1907604 Glutamate NMDA receptor; GRIN1/GRIN2A PROTEIN COMPLEX

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1201461 DEXTROMETHORPHAN POLISTIREX Glutamate [NMDA] receptor subunit epsilon 1 antagonist 4 PubMed
CHEMBL1256818 DEXTROMETHORPHAN HYDROBROMIDE MONOHYDRATE Glutamate [NMDA] receptor subunit epsilon 1 antagonist 4 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000183454
Ensembl ENSG00000183454
GO Cellular Component GO:0005783 (endoplasmic reticulum)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0008021 (synaptic vesicle)
GO:0009986 (cell surface)
GO:0014069 (postsynaptic density)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0017146 (NMDA selective glutamate receptor complex)
GO:0030054 (cell junction)
GO:0042734 (presynaptic membrane)
GO:0043005 (neuron projection)
GO:0045202 (synapse)
GO:0045211 (postsynaptic membrane)
GO Molecular Function GO:0004872 (receptor activity)
GO:0004970 (ionotropic glutamate receptor activity)
GO:0004972 (NMDA glutamate receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005216 (ion channel activity)
GO:0005234 (extracellular-glutamate-gated ion channel activity)
GO:0005261 (cation channel activity)
GO:0005262 (calcium channel activity)
GO:0005515 (protein binding)
GO:0008270 (zinc ion binding)
GO:0046872 (metal ion binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001964 (startle response)
GO:0001975 (response to amphetamine)
GO:0006810 (transport)
GO:0006811 (ion transport)
GO:0006816 (calcium ion transport)
GO:0007215 (glutamate receptor signaling pathway)
GO:0007268 (chemical synaptic transmission)
GO:0007611 (learning or memory)
GO:0007612 (learning)
GO:0007613 (memory)
GO:0008104 (protein localization)
GO:0008542 (visual learning)
GO:0009611 (response to wounding)
GO:0019233 (sensory perception of pain)
GO:0022008 (neurogenesis)
GO:0030431 (sleep)
GO:0033058 (directional locomotion)
GO:0035235 (ionotropic glutamate receptor signaling pathway)
GO:0040011 (locomotion)
GO:0042177 (negative regulation of protein catabolic process)
GO:0042391 (regulation of membrane potential)
GO:0042417 (dopamine metabolic process)
GO:0042428 (serotonin metabolic process)
GO:0042493 (response to drug)
GO:0043065 (positive regulation of apoptotic process)
GO:0043547 (positive regulation of GTPase activity)
GO:0045471 (response to ethanol)
GO:0048167 (regulation of synaptic plasticity)
GO:0050804 (modulation of synaptic transmission)
GO:0051930 (regulation of sensory perception of pain)
GO:0060078 (regulation of postsynaptic membrane potential)
GO:0060079 (excitatory postsynaptic potential)
GO:0060291 (long-term synaptic potentiation)
GO:0070588 (calcium ion transmembrane transport)
GO:0098655 (cation transmembrane transport)
GO:1900273 (positive regulation of long-term synaptic potentiation)
Wikipedia GRIN2A

Target Cross References - Protein

canSAR Q12879
CGD Epilepsy with neurodevelopmental defects
Human Protein Atlas ENSG00000183454
IntAct Q12879
Guide to Pharmacology 456
Open Targets ENSG00000183454
PharmGKB PA28979
Pharos Q12879 (Tclin)
Reactome R-HSA-438066 (Unblocking of NMDA receptor, glutamate binding and activation.)
R-HSA-442729 (CREB phosphorylation through the activation of CaMKII.)
R-HSA-442982 (Ras activation uopn Ca2+ infux through NMDA receptor.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-8849932 (SALM protein interactions at the synapse.)
UniProt O00669 Q12879 Q17RZ6

Target Cross References - Domain

InterPro IPR001320 (Iontro_rcpt.)
IPR001508 (Iono_rcpt_met.)
IPR001828 (ANF_lig-bd_rcpt.)
IPR018884 (NMDAR2_C.)
IPR019594 (Glu/Gly-bd.)
IPR028082 (Peripla_BP_I.)
Pfam PF00060 (Lig_chan)
PF01094 (ANF_receptor)
PF10565 (NMDAR2_C)
PF10613 (Lig_chan-Glu_bd)

Target Cross References - Structure

PDBe 3NFL 5H8F 5H8H 5H8N 5H8Q 5H8R 5I2J 5I2K 5I2N
CREDO 3NFL 5H8F 5H8H 5H8N 5H8Q 5H8R 5I2J 5I2K 5I2N
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