General Information of the Protein
Protein ID
PT01829
Protein Name
Glutamate receptor 2
Secondarily
Protein Name
AMPA-selective glutamate receptor 2
GluR-B
GluR-K2
Glutamate receptor ionotropic
AMPA 2
Gene Name
GRIA2
Secondarily
Gene Name
GLUR2
Sequence
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTPHIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDGTHPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINVGNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANLGFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALTYDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNIKFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTTILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKIWNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLSKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSRAEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
AMPA receptor
Function
Receptor for glutamate that functions as a ligand-gated ion channel in the central nervous system (PubMed:31300657). It plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate. Through complex formation with NSG1, GRIP1 and STX12 controls the intracellular fate of AMPAR and the endosomal sorting of the GRIA2 subunit toward recycling and membrane targeting (By similarity).
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Uniprot ID
Primary ID:
P42262

Secondarily ID:
A8MT92
I6L997
Q96FP6
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Ensembl ID
ENSG00000120251
HGNC ID
HGNC:4572
Subcellular Location
Cell membrane
Endoplasmic reticulum membrane
Postsynaptic cell membrane
Postsynaptic density 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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0015176
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-5-methyl-7-oxothieno[2,3-c]pyridin-6-yl]propanenitrile
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C20H20FN3OS
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0015330
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-4-oxothieno[3,2-c]pyridin-5-yl]propanenitrile
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C19H18FN3OS
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0015363
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-7-fluoro-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C18H17F2N5O
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0015152
3-[2-[[5-chloro-3-(trifluoromethyl)pyrazol-1-yl]methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C15H12ClF3N6O
 1
1
IC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0014796
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C18H18FN5O
 1
1
IC50 = 22000 nM
   TI
   LI
   LO
   TS
CP0015308
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C19H20FN5O
 1
1
IC50 = 22000 nM
   TI
   LI
   LO
   TS
CP0013234
(3R)-3-[2-[[5-chloro-3-(difluoromethyl)pyrazol-1-yl]methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]butanenitrile
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C16H15ClF2N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0014797
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-4-methyl-7-oxothieno[2,3-c]pyridin-6-yl]propanenitrile
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C20H20FN3OS
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015153
3-[2-[(3-bromo-5-chloropyrazol-1-yl)methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C14H12BrClN6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015174
3-[2-[(N-ethyl-4-fluoroanilino)methyl]-7-oxothieno[2,3-c]pyridin-6-yl]propanenitrile
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C19H18FN3OS
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015175
3-[4-ethyl-2-[(N-ethyl-4-fluoroanilino)methyl]-7-oxothieno[2,3-c]pyridin-6-yl]propanenitrile
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C21H22FN3OS
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015177
3-[2-[(5-chloro-3-methylpyrazol-1-yl)methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C15H15ClN6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015178
(3S)-3-[2-[[5-chloro-3-(difluoromethyl)pyrazol-1-yl]methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]butanenitrile
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C16H15ClF2N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015179
2-[2-[(N-ethyl-4-fluoroanilino)methyl]-7-oxothieno[2,3-c]pyridin-6-yl]acetonitrile
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C18H16FN3OS
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015203
3-[2-[(3,5-dichloropyrazol-1-yl)methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C14H12Cl2N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0015329
3-[2-[[5-chloro-3-(difluoromethyl)pyrazol-1-yl]methyl]-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5-yl]propanenitrile
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C15H13ClF2N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0038052
N-[(2S)-5-(6-fluoropyridin-3-yl)-2,3-dihydro-1H-inden-2-yl]propane-2-sulfonamide
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C17H19FN2O2S
 1
1 EC50 = 2500 nM
CP0008315
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
 1
1 Ki = 260 nM
CP0036440
LY 457691
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C17H22N6O2
 1
1 Ki = 6000 nM
CP0107544
LY 458545
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C17H21N5O3
 1
1 Ki = 16000 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor AMPA 2 (GRIA2) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Diabetic neuropathy [ICD-11: 8C0Z]
Approved Drug(s) 1 Approved Drug  1
1 E-2007 Approved
Diabetic neuropathy
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01414 Glutamate receptor 2 Rattus norvegicus, Rat