General Information of the Protein
| Protein ID |
PT03542
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| Protein Name |
Glutamate receptor 1
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| Secondarily Protein Name |
AMPA-selective glutamate receptor 1
GluR-A
GluR-K1
Glutamate receptor ionotropic
AMPA 1
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| Gene Name |
GRIA1
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| Secondarily Gene Name |
GLUH1
GLUR1
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| Sequence |
MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMPLGATGL
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| Organism |
Homo sapiens, Human
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| Protein Classification |
Ion channel
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Ligand-gated ion channel
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Ionotropic glutamate receptor
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AMPA receptor
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| 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 |
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| Ensembl ID | |||||
| HGNC ID | |||||
| 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
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Map of Molecular Bioactivity Related to the Protein
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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 |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Cell Line ID: CL000470 , CHO-S
Cell Line ID: CL000006 , HEK293
Cell Line ID: CL000013 , Sf9
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
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1 |
| 1 | Ki = 1600 nM | ||
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Clinical Information about the Protein
Target 1 ( Glutamate receptor AMPA 1 (GRIA1) )
| Target Type | Successful Target | ||||
|---|---|---|---|---|---|
| Disease | 3 Target-related Diseases | 3 | |||
| 1 | Diabetic neuropathy [ICD-11: 8C0Z] | ||||
| 2 | Neurological disorder [ICD-11: 6B60] | ||||
| 3 | Alzheimer disease [ICD-11: 8A20] | ||||
| Approved Drug(s) | 1 Approved Drug | 1 | |||
| 1 | E-2007 | Approved | |||
| Clinical Trial Drug(s) | 1 Clinical Trial Drug | 1 | |||
| 1 | NBQX | Phase 1 | |||
| Discontinued Drug(s) | 1 Discontinued Drug | 1 | |||
| 1 | GYKI-52466 | Terminated | |||
Similar Protein(s) and Bioactivity Statistics
50% Identity
| Protein ID | Protein Name | Protein Organism | |
| PT02409 | Glutamate receptor 1 | Rattus norvegicus, Rat | |
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