General Information of the Protein
Protein ID
PT02409
Protein Name
Glutamate receptor 1
Secondarily
Protein Name
AMPA-selective glutamate receptor 1
GluR-A
GluR-K1
Glutamate receptor ionotropic
AMPA 1
Gene Name
GRIA1
Secondarily
Gene Name
Glur1
Sequence
MPYIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQEALISIIDHYKWQTFVYIYDADRGLSVLQRVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIVKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPARIMQQWRTSDSRDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASGGGGSGENGRVVSQDFPKSMQSIPCMSHSSGMPLGATGL
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Organism
Rattus norvegicus, Rat
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
AMPA receptor
Function
Ionotropic glutamate receptor. 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
P19490
Ensembl ID
ENSG00000155511
Subcellular Location
Cell membrane
Endoplasmic reticulum membrane
Postsynaptic cell membrane
Postsynaptic density membrane
Cell projection
Dendrite
Cell projection
Dendritic spine
Early endosome membrane
Recycling endosome membrane
Presynapse
Synapse
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: CL000544 , CREM010i-SS9-1
Compound ID Compound Name Compound Formula
CP0106623
(2S)-2-amino-3-(3-hydroxy-5-methyl-1,2-oxazol-4-yl)propanoic acid
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C7H10N2O4
 1
1
Ki = 22 nM
   TI
   LI
   LO
   TS
CP0299289
(R,S)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionate
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C6H7ClN2O4
 1
1
Ki = 130 nM
   TI
   LI
   LO
   TS
CP0346493
(7S)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-7-carboxylic acid
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C7H8N2O4
 1
1
Ki = 180 nM
   TI
   LI
   LO
   TS
CP0758534
(R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid
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C7H8N2O4
 1
1
Ki = 360 nM
   TI
   LI
   LO
   TS
CP0347808
(S)-Amino-(3-hydroxy-isoxazol-5-yl)-acetic acid
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C5H6N2O4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0008940
(R,S)-alpha-amino-3-hydroxy-5-methyl-4-isooxazole-propionic acid
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C7H10N2O4
 1
1 IC50 = 40 nM
CP0299289
(R,S)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionate
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C6H7ClN2O4
 1
1 IC50 = 220 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT03542 Glutamate receptor 1 Homo sapiens, Human