General Information of the Protein
Protein ID
PT03594
Protein Name
Glutamate receptor ionotropic, kainate 5
Secondarily
Protein Name
Excitatory amino acid receptor 2
Glutamate receptor KA-2
Gene Name
GRIK5
Secondarily
Gene Name
GRIK2
Sequence
MPAELLLLLIVAFASPSCQVLSSLRMAAILDDQTVCGRGERLALALAREQINGIIEVPAKARVEVDIFELQRDSQYETTDTMCQILPKGVVSVLGPSSSPASASTVSHICGEKEIPHIKVGPEETPRLQYLRFASVSLYPSNEDVSLAVSRILKSFNYPSASLICAKAECLLRLEELVRGFLISKETLSVRMLDDSRDPTPLLKEIRDDKVSTIIIDANASISHLILRKASELGMTSAFYKYILTTMDFPILHLDGIVEDSSNILGFSMFNTSHPFYPEFVRSLNMSWRENCEASTYLGPALSAALMFDAVHVVVSAVRELNRSQEIGVKPLACTSANIWPHGTSLMNYLRMVEYDGLTGRVEFNSKGQRTNYTLRILEKSRQGHREIGVWYSNRTLAMNATTLDINLSQTLANKTLVVTTILENPYVMRRPNFQALSGNERFEGFCVDMLRELAELLRFRYRLRLVEDGLYGAPEPNGSWTGMVGELINRKADLAVAAFTITAEREKVIDFSKPFMTLGISILYRVHMGRKPGYFSFLDPFSPAVWLFMLLAYLAVSCVLFLAARLSPYEWYNPHPCLRARPHILENQYTLGNSLWFPVGGFMQQGSEIMPRALSTRCVSGVWWAFTLIIISSYTANLAAFLTVQRMEVPVESADDLADQTNIEYGTIHAGSTMTFFQNSRYQTYQRMWNYMQSKQPSVFVKSTEEGIARVLNSRYAFLLESTMNEYHRRLNCNLTQIGGLLDTKGYGIGMPLGSPFRDEITLAILQLQENNRLEILKRKWWEGGRCPKEEDHRAKGLGMENIGGIFIVLICGLIIAVFVAVMEFIWSTRRSAESEEVSVCQEMLQELRHAVSCRKTSRSRRRRRPGGPSRALLSLRAVREMRLSNGKLYSAGAGGDAGSAHGGPQRLLDDPGPPSGARPAAPTPCTHVRVCQECRRIQALRASGAGAPPRGLGVPAEATSPPRPRPGPAGPRELAEHE
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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. 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 kainate > quisqualate > domoate > L-glutamate >> AMPA >> NMDA = 1S,3R-ACPD.
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Uniprot ID
Primary ID:
Q16478

Secondarily ID:
Q8WWG8
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HGNC ID
HGNC:4583
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0402109
 Compound Info 
(S)-2-Amino-3-(5-iodo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-propionic acid
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C7H8IN3O4
  1
1
Ki = 0.24 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0437418
 Compound Info 
(S)-2-Amino-3-(6-bromo-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl)-propionic acid
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C6H7BrN4O4
  1
1
Ki = 2.9 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0373333
 Compound Info 
(S)-2-Amino-3-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-propionic acid
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C7H8BrN3O4
  1
1
Ki = 9.1 nM
 Bioactivity Info 
   TI
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CP0398465
 Compound Info 
(S)-2-Amino-3-(6-iodo-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl)-propionic acid
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C6H7IN4O4
  1
1
Ki = 19.8 nM
 Bioactivity Info 
   TI
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CP0379104
 Compound Info 
(S)-2-Amino-3-(6-chloro-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl)-propionic acid
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C6H7ClN4O4
  1
1
Ki = 30.9 nM
 Bioactivity Info 
   TI
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CP0393662
 Compound Info 
(S)-2-Amino-3-(5-chloro-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-propionic acid
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C7H8ClN3O4
  1
1
Ki = 57.1 nM
 Bioactivity Info 
   TI
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CP0000105
 Compound Info 
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
  2
1
Ki = 80 nM
 Bioactivity Info 
   TI
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2
Ki = 177 nM
 Bioactivity Info 
   TI
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CP0392797
 Compound Info 
(S)-2-Amino-3-(5-nitro-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-propionic acid
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C7H8N4O6
  1
1
Ki = 393 nM
 Bioactivity Info 
   TI
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CP0002355
 Compound Info 
(2S)-2-aminopentanedioic acid
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C5H9NO4
  2
1
Ki = 701 nM
 Bioactivity Info 
   TI
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2
Ki = 750 nM
 Bioactivity Info 
   TI
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CP0469374
 Compound Info 
(S)-2-Amino-3-(6-methyl-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl)-propionic acid
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C7H10N4O4
  1
1
Ki = 1150 nM
 Bioactivity Info 
   TI
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CP0331934
 Compound Info 
(6-Nitro-2,3-dioxo-7-pyrrol-1-yl-3,4-dihydro-2H-quinoxalin-1-yl)-acetic acid
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C14H10N4O6
  1
1
Ki = 1300 nM
 Bioactivity Info 
   TI
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CP0373040
 Compound Info 
(S)-2-Amino-3-(5-fluoro-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-propionic acid
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C7H8FN3O4
  1
1
Ki = 1820 nM
 Bioactivity Info 
   TI
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CP0419091
 Compound Info 
(S)-2-Amino-3-(3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl)-propionic acid
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C6H8N4O4
  1
1
Ki = 1980 nM
 Bioactivity Info 
   TI
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CP0106623
 Compound Info 
(2S)-2-amino-3-(3-hydroxy-5-methyl-1,2-oxazol-4-yl)propanoic acid
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C7H10N2O4
  1
1
Ki = 2144 nM
 Bioactivity Info 
   TI
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CP0376766
 Compound Info 
(2S,4E)-2-amino-4-(2-methylpropylidene)pentanedioic acid
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C9H15NO4
  1
1
Ki = 7500 nM
 Bioactivity Info 
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CP0161087
 Compound Info 
(3S,4aR,6S,8aR)-6-[[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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C16H24F2N2O4
  1
1
Ki = 8900 nM
 Bioactivity Info 
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CP0377460
 Compound Info 
(2S,4R)-2-amino-4-[(E)-3-(2-methoxyphenyl)prop-2-enyl]pentanedioic acid
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C15H19NO5
  1
1
Ki > 10000 nM
 Bioactivity Info 
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CP0067501
 Compound Info 
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
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CP0460278
 Compound Info 
(S)-2-Amino-4-cyclopentylidene-pentanedioic acid
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C10H15NO4
  1
1
Ki = 10000 nM
 Bioactivity Info 
   TI
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CP0457282
 Compound Info 
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 = 18000 nM
 Bioactivity Info 
   TI
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CP0451571
 Compound Info 
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 = 20000 nM
 Bioactivity Info 
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CP0453155
 Compound Info 
(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 = 20000 nM
 Bioactivity Info 
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CP0373526
 Compound Info 
(S)-2-Amino-4-(1-ethyl-propylidene)-pentanedioic acid
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C10H17NO4
  1
1
Ki = 21400 nM
 Bioactivity Info 
   TI
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CP0200335
 Compound Info 
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 = 25000 nM
 Bioactivity Info 
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CP0397255
 Compound Info 
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 = 25000 nM
 Bioactivity Info 
   TI
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CP0252279
 Compound Info 
(2S)-2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid
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C7H9N3O4
  1
1
Ki = 28900 nM
 Bioactivity Info 
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CP0395220
 Compound Info 
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 > 30000 nM
 Bioactivity Info 
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CP0398226
 Compound Info 
3-(7-{3-[(Benzyl-methyl-amino)-methyl]-pyrrol-1-yl}-6-nitro-2,3-dioxo-3,4-dihydro-2H-quinoxalin-1-yl)-propionic acid
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C24H23N5O6
  1
1
Ki > 30000 nM
 Bioactivity Info 
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CP0399794
 Compound Info 
(2S,4Z)-2-amino-4-(2-methylpropylidene)pentanedioic acid
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C9H15NO4
  1
1
Ki = 82200 nM
 Bioactivity Info 
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000105
 Compound Info 
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
  1
1 Ki = 8 nM
CP0002355
 Compound Info 
(2S)-2-aminopentanedioic acid
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C5H9NO4
  1
1 Ki = 750 nM
CP0067501
 Compound Info 
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
  1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic kainate 5 (GRIK5) )
Target Type Literature-reported Target