General Information of the Protein
Protein ID
PT01407
Protein Name
Glutamate receptor 3
Secondarily
Protein Name
AMPA-selective glutamate receptor 3
GluR-C
GluR-K3
Glutamate receptor ionotropic
AMPA 3
Gene Name
GRIA3
Secondarily
Gene Name
GLUR3
GLURC
Sequence
MARQKKMGQSVLRAVFFLVLGLLGHSHGGFPNTISIGGLFMRNTVQEHSAFRFAVQLYNTNQNTTEKPFHLNYHVDHLDSSNSFSVTNAFCSQFSRGVYAIFGFYDQMSMNTLTSFCGALHTSFVTPSFPTDADVQFVIQMRPALKGAILSLLGHYKWEKFVYLYDTERGFSILQAIMEAAVQNNWQVTARSVGNIKDVQEFRRIIEEMDRRQEKRYLIDCEVERINTILEQVVILGKHSRGYHYMLANLGFTDILLERVMHGGANITGFQIVNNENPMVQQFIQRWVRLDEREFPEAKNAPLKYTSALTHDAILVIAEAFRYLRRQRVDVSRRGSAGDCLANPAVPWSQGIDIERALKMVQVQGMTGNIQFDTYGRRTNYTIDVYEMKVSGSRKAGYWNEYERFVPFSDQQISNDSASSENRTIVVTTILESPYVMYKKNHEQLEGNERYEGYCVDLAYEIAKHVRIKYKLSIVGDGKYGARDPETKIWNGMVGELVYGRADIAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHLEDNNEEPRDPQSPPDPPNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLDSGSTKEFFRRSKIAVYEKMWSYMKSAEPSVFTKTTADGVARVRKSKGKFAFLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGVATPKGSALRNAVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILVGGLGLAMMVALIEFCYKSRAESKRMKLTKNTQNFKPAPATNTQNYATYREGYNVYGTESVKI
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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 and 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.
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Uniprot ID
Primary ID:
P42263

Secondarily ID:
D3DTF1
Q4VXD5
Q4VXD6
Q9HDA0
Q9HDA1
Q9HDA2
Q9P0H1
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Ensembl ID
ENSG00000125675
HGNC ID
HGNC:4573
Subcellular Location
Cell membrane
Postsynaptic cell 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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0470950
N-[2-[4-(4-cyanophenyl)cyclohexyl]propyl]propane-2-sulfonamide
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C19H28N2O2S
 1
1
EC50 = 1660 nM
   TI
   LI
   LO
   TS
CP0374874
(+/-) Propane-2-sulfonic acid [2-(4'-cyano-biphenyl-4-yl)-propyl]-amide
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C19H22N2O2S
 1
1
EC50 = 1660 nM
   TI
   LI
   LO
   TS
CP0000104
3-Bicyclo[2.2.1]hept-5-en-2-yl-6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[1,2,4]thiadiazine-7-sulfonic acid amide
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C14H16ClN3O4S2
 1
1
EC50 = 13700 nM
   TI
   LI
   LO
   TS
CP0008315
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
 1
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0162369
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid
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C14H10BrClN2O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0374730
4-Chloro-2-(3-naphthalen-2-yl-ureido)-benzoic acid
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C18H13ClN2O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0204536
(2S,4R)-2-amino-4-[(E)-3-(4-chlorophenyl)prop-2-enyl]pentanedioic acid
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C14H16ClNO4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0008315
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
 1
1 Ki = 900 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor AMPA 3 (GRIA3) )
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
90% Identity
Protein ID Protein Name Protein Organism
PT03116 Glutamate receptor 3 Rattus norvegicus, Rat