General Information of the Protein
Protein ID
PT02751
Protein Name
Glutamate receptor ionotropic, NMDA 2B
Secondarily
Protein Name
Glutamate [NMDA] receptor subunit epsilon-2
N-methyl D-aspartate receptor subtype 2B
N-methyl-D-aspartate receptor subunit 3
Gene Name
GRIN2B
Secondarily
Gene Name
NMDAR2B
Sequence
MKPRAECCSPKFWLVLAVLAVSGSRARSQKSPPSIGIAVILVGTSDEVAIKDAHEKDDFHHLSVVPRVELVAMNETDPKSIITRICDLMSDRKIQGVVFADDTDQEAIAQILDFISAQTLTPILGIHGGSSMIMADKDESSMFFQFGPSIEQQASVMLNIMEEYDWYIFSIVTTYFPGYQDFVNKIRSTIENSFVGWELEEVLLLDMSLDDGDSKIQNQLKKLQSPIILLYCTKEEATYIFEVANSVGLTGYGYTWIVPSLVAGDTDTVPAEFPTGLISVSYDEWDYGLPARVRDGIAIITTAASDMLSEHSFIPEPKSSCYNTHEKRIYQSNMLNRYLINVTFEGRNLSFSEDGYQMHPKLVIILLNKERKWERVGKWKDKSLQMKYYVWPRMCPETEEQEDDHLSIVTLEEAPFVIVESVDPLSGTCMRNTVPCQKRIVTENKTDEEPGYIKKCCKGFCIDILKKISKSVKFTYDLYLVTNGKHGKKINGTWNGMIGEVVMKRAYMAVGSLTINEERSEVVDFSVPFIETGISVMVSRSNGTVSPSAFLEPFSADVWVMMFVMLLIVSAVAVFVFEYFSPVGYNRCLADGREPGGPSFTIGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEYVDQVSGLSDKKFQRPNDFSPPFRFGTVPNGSTERNIRNNYAEMHAYMGKFNQRGVDDALLSLKTGKLDAFIYDAAVLNYMAGRDEGCKLVTIGSGKVFASTGYGIAIQKDSGWKRQVDLAILQLFGDGEMEELEALWLTGICHNEKNEVMSSQLDIDNMAGVFYMLGAAMALSLITFICEHLFYWQFRHCFMGVCSGKPGMVFSISRGIYSCIHGVAIEERQSVMNSPTATMNNTHSNILRLLRTAKNMANLSGVNGSPQSALDFIRRESSVYDISEHRRSFTHSDCKSYNNPPCEENLFSDYISEVERTFGNLQLKDSNVYQDHYHHHHRPHSIGSASSIDGLYDCDNPPFTTQSRSISKKPLDIGLPSSKHSQLSDLYGKFSFKSDRYSGHDDLIRSDVSDISTHTVTYGNIEGNAAKRRKQQYKDSLKKRPASAKSRREFDEIELAYRRRPPRSPDHKRYFRDKEGLRDFYLDQFRTKENSPHWEHVDLTDIYKERSDDFKRDSVSGGGPCTNRSHIKHGTGDKHGVVSGVPAPWEKNLTNVEWEDRSGGNFCRSCPSKLHNYSTTVTGQNSGRQACIRCEACKKAGNLYDISEDNSLQELDQPAAPVAVTSNASTTKYPQSPTNSKAQKKNRNKLRRQHSYDTFVDLQKEEAALAPRSVSLKDKGRFMDGSPYAHMFEMSAGESTFANNKSSVPTAGHHHHNNPGGGYMLSKSLYPDRVTQNPFIPTFGDDQCLLHGSKSYFFRQPTVAGASKARPDFRALVTNKPVVSALHGAVPARFQKDICIGNQSNPCVPNNKNPRAFNGSSNGHVYEKLSSIESDV
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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:28126851). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:8768735, PubMed:26875626). In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an irreversible neuronal death. Contributes to neural pattern formation in the developing brain. Plays a role in long-term depression (LTD) of hippocampus membrane currents and in synaptic plasticity (By similarity).
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Uniprot ID
Primary ID:
Q13224

Secondarily ID:
Q12919
Q13220
Q13225
Q14CU4
Q9UM56
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Ensembl ID
ENSG00000273079
HGNC ID
HGNC:4586
Subcellular Location
Cell membrane
Postsynaptic cell membrane
Late endosome
Lysosome
Cytoplasm
Cytoskeleton
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0008860
1-((1S,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol
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C20H25NO3
 1
1
IC50 = 74 nM
   TI
   LI
   LO
   TS
CP0444070
4-[4-chloro-3-(difluoromethoxy)phenyl]-1-(1H-pyrazol-5-ylmethyl)pyrazole
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C14H11ClF2N4O
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0342282
N-[[5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl]methyl]pyrazine-2-carboxamide
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C18H15FN4O2
 1
1
IC50 = 262 nM
   TI
   LI
   LO
   TS
CP0377015
4-[4-chloro-3-(difluoromethoxy)phenyl]-1-(1H-pyrazol-4-ylmethyl)pyrazole
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C14H11ClF2N4O
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0446596
4-[3-(difluoromethoxy)-4-fluorophenyl]-1-(1H-pyrazol-5-ylmethyl)pyrazole
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C14H11F3N4O
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0075084
1-cyclopropyl-N-((6-(4-fluoro-2-methoxyphenyl)pyrazin-2-yl)methyl)methanamine
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C16H18FN3O
 1
1
IC50 = 508 nM
   TI
   LI
   LO
   TS
CP0241221
N-[[5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl]methyl]pyridine-2-carboxamide
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C19H16FN3O2
 1
1
IC50 = 673 nM
   TI
   LI
   LO
   TS
CP0199373
N-[[5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl]methyl]cyclopentanamine
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C18H21FN2O
 1
1
IC50 = 770 nM
   TI
   LI
   LO
   TS
CP0446692
4-[4-chloro-3-(difluoromethyl)phenyl]-1-(1H-pyrazol-5-ylmethyl)pyrazole
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C14H11ClF2N4
 1
1
IC50 = 890 nM
   TI
   LI
   LO
   TS
CP0493632
4-[4-chloro-3-(difluoromethoxy)phenyl]-1-[(1-methylpyrazol-4-yl)methyl]pyrazole
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C15H13ClF2N4O
 1
1
IC50 = 1750 nM
   TI
   LI
   LO
   TS
CP0510167
3-[[4-[4-chloro-3-(difluoromethoxy)phenyl]pyrazol-1-yl]methyl]-1-methylpyrazole
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C15H13ClF2N4O
 1
1
IC50 = 2460 nM
   TI
   LI
   LO
   TS
CP0446693
4-[4-chloro-3-(difluoromethoxy)phenyl]-1-[(5-ethyl-1H-pyrazol-4-yl)methyl]pyrazole
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C16H15ClF2N4O
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0047474
N'-[(2-methoxyphenyl)methyl]-4-(trifluoromethoxy)benzenecarboximidamide
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C16H15F3N2O2
 1
1 IC50 = 4.1 nM
CP0096509
N'-[(3,5-dimethylphenyl)methyl]-4-(trifluoromethoxy)benzenecarboximidamide
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C17H17F3N2O
 1
1 IC50 = 4.2 nM
CP0250776
N'-[(3,5-dimethylphenyl)methyl]-4-(trifluoromethyl)benzenecarboximidamide
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C17H17F3N2
 1
1 IC50 = 8.7 nM
CP0002756
4-((1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl)phenol
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C22H29NO2
 1
1 IC50 = 9 nM
CP0105176
N'-[(3-methoxyphenyl)methyl]-4-(trifluoromethoxy)benzenecarboximidamide
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C16H15F3N2O2
 1
1 IC50 = 9.7 nM
CP0001508
(+/-)-[2-(4-benzylpiperidino)-1-(4-hydroxyphenyl)-1-propanol]
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C21H27NO2
 1
1 IC50 = 20 nM
CP0250099
N'-[(3,5-dichlorophenyl)methyl]-4-(trifluoromethoxy)benzenecarboximidamide
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C15H11Cl2F3N2O
 1
1 IC50 = 24 nM
CP0277254
N'-[(3-chlorophenyl)methyl]-4-(trifluoromethyl)benzenecarboximidamide
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C15H12ClF3N2
 1
1 IC50 = 32 nM
CP0276489
N'-benzyl-4-(trifluoromethoxy)benzenecarboximidamide
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C15H13F3N2O
 1
1 IC50 = 46 nM
CP0055493
4-trifluoromethoxy-N-(2-trifluoromethyl-benzyl)-benzamidine
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C16H12F6N2O
 2
1 IC50 = 47 nM
2 Ki = 72 nM
CP0497275
N'-[(2-chlorophenyl)methyl]-4-(trifluoromethyl)benzenecarboximidamide
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C15H12ClF3N2
 1
1 IC50 = 48 nM
CP0102292
3,4-Dichloro-N-(2-trifluoromethoxy-benzyl)-benzamidine
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C15H11Cl2F3N2O
 1
1 IC50 = 57 nM
CP0206005
3,4-Dichloro-N-(3-chloro-benzyl)-benzamidine
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C14H11Cl3N2
 1
1 IC50 = 110 nM
CP0306822
4-Chloro-N-(3-chloro-benzyl)-benzamidine
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C14H12Cl2N2
 1
1 IC50 = 160 nM
CP0080607
N'-benzyl-4-(trifluoromethyl)benzenecarboximidamide
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C15H13F3N2
 1
1 IC50 = 360 nM
CP0274494
3-Chloro-N-(3-chloro-benzyl)-benzamidine
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C14H12Cl2N2
 1
1 IC50 = 420 nM
CP0333027
N'-[(3-chlorophenyl)methyl]-4-fluorobenzenecarboximidamide
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C14H12ClFN2
 1
1 IC50 = 450 nM
CP0302849
4-Trifluoromethyl-N-(3-trifluoromethyl-benzyl)-benzamidine
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C16H12F6N2
 1
1 IC50 = 660 nM
CP0333062
N'-benzyl-4-chlorobenzenecarboximidamide
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C14H13ClN2
 1
1 IC50 = 720 nM
CP0634104
(E)-N-(2-Methoxy-benzyl)-3-phenyl-acrylamidine
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C17H18N2O
 1
1 Kd = 1 nM
CP0002005
(+)-erythro 4-[2-(4-Benzyl-piperidin-1-yl)-1-hydroxy-propyl]-phenol
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C21H27NO2
 1
1 Kd = 94 nM
CP0634009
(E)-N1-(benzyl)cinnamamidine
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C16H16N2
 1
1 Ki = 9 nM
CP0264018
(5S,7S)-2-methoxy-7-(3-phenylpropylamino)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol
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C21H27NO2
 1
1 Ki = 16 nM
CP0913653
trans-2-methoxy-7-(3-phenylpropylamino)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol
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C21H27NO2
 1
1 Ki = 48 nM
CP0004824
N'-benzylbenzenecarboximidamide
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C14H14N2
 1
1 Ki = 10000 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic NMDA 2B (NMDAR2B) )
Target Type Successful Target
Disease 9 Target-related Diseases  9
1 Alpha-1 antitrypsin deficiency [ICD-11: 5C5A]
2 Major depressive disorder [ICD-11: 6A70.3]
3 Multiple sclerosis [ICD-11: 8A40]
4 Peripheral neuropathy [ICD-11: 8C0Z]
5 Neurological disorder [ICD-11: 6B60]
6 Parkinson disease [ICD-11: 8A00.0]
7 Cerebrovascular ischaemia [ICD-11: 8B1Z]
8 Alzheimer disease [ICD-11: 8A20]
9 Cancer related pain [ICD-11: MG30]
Approved Drug(s) 1 Approved Drug  1
1 Alpha 1-PI Approved
Alpha-1 antitrypsin deficiency
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 CERC-301 Phase 2
Major depressive disorder
2 ELIPRODIL Phase 2
Multiple sclerosis
3 RGH-896 Phase 2
Peripheral neuropathy
4 NBQX Phase 1
Neurological disorder
5 CP-101,606 Phase 2
Parkinson disease
Discontinued Drug(s) 6 Discontinued Drugs  6
1 Besonprodil Discontinued in Phase 1
Parkinson disease
2 DIZOCILPINE Terminated
Cerebrovascular ischaemia
3 L-698532 Terminated
Neurological disorder
4 L-698544 Terminated
Alzheimer disease
5 L-701324 Terminated
Cerebrovascular ischaemia
6 RO-25-6981 Terminated
Cancer related pain
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06444 Glutamate receptor ionotropic, NMDA 2B Mus musculus, Mouse