General Information of the Protein
Protein ID
PT04248
Protein Name
Glutamate receptor ionotropic, NMDA 2A
Secondarily
Protein Name
Glutamate [NMDA] receptor subunit epsilon-1
N-methyl D-aspartate receptor subtype 2A
Gene Name
GRIN2A
Secondarily
Gene Name
NMDAR2A
Sequence
MGRVGYWTLLVLPALLVWRGPAPSAAAEKGPPALNIAVMLGHSHDVTERELRTLWGPEQAAGLPLDVNVVALLMNRTDPKSLITHVCDLMSGARIHGLVFGDDTDQEAVAQMLDFISSHTFVPILGIHGGASMIMADKDPTSTFFQFGASIQQQATVMLKIMQDYDWHVFSLVTTIFPGYREFISFVKTTVDNSFVGWDMQNVITLDTSFEDAKTQVQLKKIHSSVILLYCSKDEAVLILSEARSLGLTGYDFFWIVPSLVSGNTELIPKEFPSGLISVSYDDWDYSLEARVRDGIGILTTAASSMLEKFSYIPEAKASCYGQMERPEVPMHTLHPFMVNVTWDGKDLSFTEEGYQVHPRLVVIVLNKDREWEKVGKWENHTLSLRHAVWPRYKSFSDCEPDDNHLSIVTLEEAPFVIVEDIDPLTETCVRNTVPCRKFVKINNSTNEGMNVKKCCKGFCIDILKKLSRTVKFTYDLYLVTNGKHGKKVNNVWNGMIGEVVYQRAVMAVGSLTINEERSEVVDFSVPFVETGISVMVSRSNGTVSPSAFLEPFSASVWVMMFVMLLIVSAIAVFVFEYFSPVGYNRNLAKGKAPHGPSFTIGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEFVDQVTGLSDKKFQRPHDYSPPFRFGTVPNGSTERNIRNNYPYMHQYMTKFNQKGVEDALVSLKTGKLDAFIYDAAVLNYKAGRDEGCKLVTIGSGYIFATTGYGIALQKGSPWKRQIDLALLQFVGDGEMEELETLWLTGICHNEKNEVMSSQLDIDNMAGVFYMLAAAMALSLITFIWEHLFYWKLRFCFTGVCSDRPGLLFSISRGIYSCIHGVHIEEKKKSPDFNLTGSQSNMLKLLRSAKNISSMSNMNSSRMDSPKRAADFIQRGSLIMDMVSDKGNLMYSDNRSFQGKESIFGDNMNELQTFVANRQKDNLNNYVFQGQHPLTLNESNPNTVEVAVSTESKANSRPRQLWKKSVDSIRQDSLSQNPVSQRDEATAENRTHSLKSPRYLPEEMAHSDISETSNRATCHREPDNSKNHKTKDNFKRSVASKYPKDCSEVERTYLKTKSSSPRDKIYTIDGEKEPGFHLDPPQFVENVTLPENVDFPDPYQDPSENFRKGDSTLPMNRNPLHNEEGLSNNDQYKLYSKHFTLKDKGSPHSETSERYRQNSTHCRSCLSNMPTYSGHFTMRSPFKCDACLRMGNLYDIDEDQMLQETGNPATGEQVYQQDWAQNNALQLQKNKLRISRQHSYDNIVDKPRELDLSRPSRSISLKDRERLLEGNFYGSLFSVPSSKLSGKKSSLFPQGLEDSKRSKSLLPDHTSDNPFLHSHRDDQRLVIGRCPSDPYKHSLPSQAVNDSYLRSSLRSTASYCSRDSRGHNDVYISEHVMPYAANKNNMYSTPRVLNSCSNRRVYKKMPSIESDV
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
NMDA receptor
Function
Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:8768735, PubMed:26919761, PubMed:26875626, PubMed:28105280). Sensitivity to glutamate and channel kinetics depend on the subunit composition; channels containing GRIN1 and GRIN2A have lower sensitivity to glutamate and faster deactivation kinetics than channels formed by GRIN1 and GRIN2B (PubMed:26919761, PubMed:26875626). Contributes to the slow phase of excitatory postsynaptic current, long-term synaptic potentiation, and learning (By similarity).
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Uniprot ID
Primary ID:
Q12879

Secondarily ID:
O00669
Q17RZ6
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Ensembl ID
ENSG00000183454
HGNC ID
HGNC:4585
Subcellular Location
Cell projection
Dendritic spine
Cell membrane
Synapse
Postsynaptic cell membrane
Cytoplasmic vesicle membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000041 , LTK-
Compound ID Compound Name Compound Formula
CP0419689
benzyl 4-[(pyridin-4-ylamino)methyl]piperidine-1-carboxylate
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C19H23N3O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0185104
N-[2-(4-phenylmethoxyphenyl)ethyl]pyridin-4-amine
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C20H20N2O
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic NMDA 2A (NMDAR2A) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Malnutrition [ICD-11: 5B50-5B71]
2 Neurological disorder [ICD-11: 6B60]
3 Cerebrovascular ischaemia [ICD-11: 8B1Z]
4 Alzheimer disease [ICD-11: 8A20]
Approved Drug(s) 1 Approved Drug  1
1 Glycine Approved
Malnutrition
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 NBQX Phase 1
Neurological disorder
Discontinued Drug(s) 4 Discontinued Drugs  4
1 DIZOCILPINE Terminated
Cerebrovascular ischaemia
2 L-698532 Terminated
Neurological disorder
3 L-698544 Terminated
Alzheimer disease
4 L-701324 Terminated
Cerebrovascular ischaemia