General Information of the Protein
Protein ID
PT04971
Protein Name
Glutamate receptor ionotropic, kainate 3
Secondarily
Protein Name
Excitatory amino acid receptor 5
Glutamate receptor 7
Gene Name
GRIK3
Secondarily
Gene Name
GLUR7
Sequence
MTAPWRRLRSLVWEYWAGLLVCAFWIPDSRGMPHVIRIGGIFEYADGPNAQVMNAEEHAFRFSANIINRNRTLLPNTTLTYDIQRIHFHDSFEATKKACDQLALGVVAIFGPSQGSCTNAVQSICNALEVPHIQLRWKHHPLDNKDTFYVNLYPDYASLSHAILDLVQYLKWRSATVVYDDSTGLIRLQELIMAPSRYNIRLKIRQLPIDSDDSRPLLKEMKRGREFRIIFDCSHTMAAQILKQAMAMGMMTEYYHFIFTTLDLYALDLEPYRYSGVNLTGFRILNVDNPHVSAIVEKWSMERLQAAPRSESGLLDGVMMTDAALLYDAVHIVSVCYQRAPQMTVNSLQCHRHKAWRFGGRFMNFIKEAQWEGLTGRIVFNKTSGLRTDFDLDIISLKEDGLEKVGVWSPADGLNITEVAKGRGPNVTDSLTNRSLIVTTVLEEPFVMFRKSDRTLYGNDRFEGYCIDLLKELAHILGFSYEIRLVEDGKYGAQDDKGQWNGMVKELIDHKADLAVAPLTITHVREKAIDFSKPFMTLGVSILYRKPNGTNPSVFSFLNPLSPDIWMYVLLAYLGVSCVLFVIARFSPYEWYDAHPCNPGSEVVENNFTLLNSFWFGMGSLMQQGSELMPKALSTRIIGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVKDGATMTFFKKSKISTFEKMWAFMSSKPSALVKNNEEGIQRALTADYALLMESTTIEYVTQRNCNLTQIGGLIDSKGYGIGTPMGSPYRDKITIAILQLQEEDKLHIMKEKWWRGSGCPEEENKEASALGIQKIGGIFIVLAAGLVLSVLVAVGEFVYKLRKTAEREQRSFCSTVADEIRFSLTCQRRVKHKPQPPMMVKTDAVINMHTFNDRRLPGKDSMACSTSLAPVFP
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
Kainate 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. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists. This receptor binds domoate > kainate >> L-glutamate = quisqualate >> AMPA = NMDA.
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Uniprot ID
Primary ID:
Q13003

Secondarily ID:
A9Z1Z8
B1AMS6
Q13004
Q16136
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HGNC ID
HGNC:4581
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
CP0008315
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
 2
1
IC50 = 44000 nM
   TI
   LI
   LO
   TS
2
Ki = 18000 nM
   TI
   LI
   LO
   TS
CP0000105
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0377460
(2S,4R)-2-amino-4-[(E)-3-(2-methoxyphenyl)prop-2-enyl]pentanedioic acid
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C15H19NO5
 1
1
Ki = 42 nM
   TI
   LI
   LO
   TS
CP0207002
(7-{3-[3-(4-Nitro-phenyl)-ureidomethyl]-pyrrol-1-yl}-2,3-dioxo-6-trifluoromethyl-3,4-dihydro-2H-quinoxalin-1-yl)-acetic acid
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C23H17F3N6O7
 1
1
Ki = 46 nM
   TI
   LI
   LO
   TS
CP0376766
(2S,4E)-2-amino-4-(2-methylpropylidene)pentanedioic acid
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C9H15NO4
 1
1
Ki = 518 nM
   TI
   LI
   LO
   TS
CP0457282
2-[6-nitro-2,3-dioxo-7-[3-[(4-phenylpiperidin-1-yl)methyl]pyrrol-1-yl]-4H-quinoxalin-1-yl]acetic acid
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C26H25N5O6
 1
1
Ki = 530 nM
   TI
   LI
   LO
   TS
CP0067501
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
 1
1
Ki = 617 nM
   TI
   LI
   LO
   TS
CP0451571
2-[7-[3-[(4-benzylpiperazin-1-yl)methyl]pyrrol-1-yl]-6-nitro-2,3-dioxo-4H-quinoxalin-1-yl]acetic acid
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C26H26N6O6
 1
1
Ki = 680 nM
   TI
   LI
   LO
   TS
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 1
1
Ki = 789 nM
   TI
   LI
   LO
   TS
CP0397255
2-[6-nitro-2,3-dioxo-7-[3-[[4-(2-phenylethyl)piperazin-1-yl]methyl]pyrrol-1-yl]-4H-quinoxalin-1-yl]acetic acid
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C27H28N6O6
 1
1
Ki = 1400 nM
   TI
   LI
   LO
   TS
CP0453155
(6-Nitro-2,3-dioxo-7-{3-[(3-phenyl-propylamino)-methyl]-pyrrol-1-yl}-3,4-dihydro-2H-quinoxalin-1-yl)-acetic acid
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C24H23N5O6
 1
1
Ki = 1400 nM
   TI
   LI
   LO
   TS
CP0200335
3-(6-Nitro-2,3-dioxo-7-pyrrol-1-yl-3,4-dihydro-2H-quinoxalin-1-yl)-propionic acid
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C15H12N4O6
 1
1
Ki = 2500 nM
   TI
   LI
   LO
   TS
CP0087609
1-(4-Carboxymethyl-7-nitro-2,3-dioxo-1,2,3,4-tetrahydro-quinoxalin-6-yl)-1H-pyrrole-3-carboxylic acid
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C15H10N4O8
 1
1
Ki = 4100 nM
   TI
   LI
   LO
   TS
CP0395220
2-[6-nitro-2,3-dioxo-7-[3-(piperidin-1-ylmethyl)pyrrol-1-yl]-4H-quinoxalin-1-yl]acetic acid
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C20H21N5O6
 1
1
Ki = 5700 nM
   TI
   LI
   LO
   TS
CP0460278
(S)-2-Amino-4-cyclopentylidene-pentanedioic acid
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C10H15NO4
 1
1
Ki = 5730 nM
   TI
   LI
   LO
   TS
CP0399794
(2S,4Z)-2-amino-4-(2-methylpropylidene)pentanedioic acid
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C9H15NO4
 1
1
Ki = 10500 nM
   TI
   LI
   LO
   TS
CP0373526
(S)-2-Amino-4-(1-ethyl-propylidene)-pentanedioic acid
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C10H17NO4
 1
1
Ki = 12400 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000105
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
 1
1 Ki = 10 nM
CP0067501
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
 1
1 Ki = 617 nM
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 1
1 Ki = 789 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic kainate 3 (GluK3) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02970 Glutamate receptor ionotropic, kainate 3 Rattus norvegicus, Rat