General Information of the Protein
Protein ID
PT02754
Protein Name
Glutamate receptor ionotropic, kainate 2
Secondarily
Protein Name
Excitatory amino acid receptor 4
Glutamate receptor 6
Gene Name
GRIK2
Secondarily
Gene Name
GLUR6
Sequence
MKIIFPILSNPVFRRTVKLLLCLLWIGYSQGTTHVLRFGGIFEYVESGPMGAEELAFRFAVNTINRNRTLLPNTTLTYDTQKINLYDSFEASKKACDQLSLGVAAIFGPSHSSSANAVQSICNALGVPHIQTRWKHQVSDNKDSFYVSLYPDFSSLSRAILDLVQFFKWKTVTVVYDDSTGLIRLQELIKAPSRYNLRLKIRQLPADTKDAKPLLKEMKRGKEFHVIFDCSHEMAAGILKQALAMGMMTEYYHYIFTTLDLFALDVEPYRYSGVNMTGFRILNTENTQVSSIIEKWSMERLQAPPKPDSGLLDGFMTTDAALMYDAVHVVSVAVQQFPQMTVSSLQCNRHKPWRFGTRFMSLIKEAHWEGLTGRITFNKTNGLRTDFDLDVISLKEEGLEKIGTWDPASGLNMTESQKGKPANITDSLSNRSLIVTTILEEPYVLFKKSDKPLYGNDRFEGYCIDLLRELSTILGFTYEIRLVEDGKYGAQDDANGQWNGMVRELIDHKADLAVAPLAITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYILLAYLGVSCVLFVIARFSPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVEDGATMTFFKKSKISTYDKMWAFMSSRRQSVLVKSNEEGIQRVLTSDYAFLMESTTIEFVTQRNCNLTQIGGLIDSKGYGVGTPMGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEESKEASALGVQNIGGIFIVLAAGLVLSVFVAVGEFLYKSKKNAQLEKRSFCSAMVEELRMSLKCQRRLKHKPQAPVIVKTEEVINMHTFNDRRLPGKETMA
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
Kainate 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 (PubMed:28180184). Modulates cell surface expression of NETO2 (By similarity).
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Uniprot ID
Primary ID:
Q13002

Secondarily ID:
A6NMY9
B5MCV0
D7RWZ3
D7RWZ4
D7RWZ5
D7RWZ6
D7RWZ7
Q8WWS1
Q96KS6
Q96KS7
Q96KS8
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Ensembl ID
ENSG00000164418
HGNC ID
HGNC:4580
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
CP0000105
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
 3
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
2
Ki = 32 nM
   TI
   LI
   LO
   TS
3
Ki = 32.4 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
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0397866
(2S,4R)-4-allyl glutamate
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C8H13NO4
 2
1
EC50 = 8300 nM
   TI
   LI
   LO
   TS
2
Ki = 1840 nM
   TI
   LI
   LO
   TS
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 2
1
EC50 = 25000 nM
   TI
   LI
   LO
   TS
2
Ki = 1106 nM
   TI
   LI
   LO
   TS
CP0383813
2-Amino-4-but-2-enyl-pentanedioic acid(LY339180)
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C9H15NO4
 2
1
EC50 = 58300 nM
   TI
   LI
   LO
   TS
2
Ki = 3258 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
 3
1
EC50 = 70800 nM
   TI
   LI
   LO
   TS
2
Ki = 3859 nM
   TI
   LI
   LO
   TS
3
Ki = 4649 nM
   TI
   LI
   LO
   TS
CP0067501
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
 5
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 13723 nM
   TI
   LI
   LO
   TS
4
Ki = 15406 nM
   TI
   LI
   LO
   TS
5
Ki = 15410 nM
   TI
   LI
   LO
   TS
CP0460278
(S)-2-Amino-4-cyclopentylidene-pentanedioic acid
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C10H15NO4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0378727
1-(3-bromophenyl)-3-[5-chloro-2-(1H-tetrazol-5-yl-phenyl]urea
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C14H10BrClN6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0162369
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid
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C14H10BrClN2O3
 1
1
IC50 = 28000 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 = 29000 nM
   TI
   LI
   LO
   TS
CP0051516
1-[5-chloro-2-(5-oxo-4,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-3-(3-bromophenyl)urea
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C15H10BrClN4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0312285
2-[3-(3-bromophenyl)ureido]-4-chlorobenzenesulfonic acid
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C13H10BrClN2O4S
 1
1
IC50 = 37000 nM
   TI
   LI
   LO
   TS
CP0346386
2-[2-[(3-bromophenyl)carbamoylamino]-4-chlorophenyl]acetic acid
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C15H12BrClN2O3
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0374730
4-Chloro-2-(3-naphthalen-2-yl-ureido)-benzoic acid
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C18H13ClN2O3
 1
1
IC50 = 62000 nM
   TI
   LI
   LO
   TS
CP0040797
(2S,4R)-2-Amino-4-methyl-pentanedioic acid
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C6H11NO4
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0161087
(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 = 50 nM
   TI
   LI
   LO
   TS
CP0470502
2-Amino-4-prop-2-ynyl-pentanedioic acid
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C8H11NO4
 1
1
Ki = 160 nM
   TI
   LI
   LO
   TS
CP0397871
(2S,4R)-2-amino-4-[(Z)-3-phenylprop-2-enyl]pentanedioic acid
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C14H17NO4
 1
1
Ki = 339 nM
   TI
   LI
   LO
   TS
CP0289436
(2S)-2-amino-4-methylidenepentanedioic acid
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C6H9NO4
 1
1
Ki = 450 nM
   TI
   LI
   LO
   TS
CP0384180
2-Amino-4-(2-methyl-3-phenyl-allyl)-pentanedioic acid
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C15H19NO4
 1
1
Ki = 500 nM
   TI
   LI
   LO
   TS
CP0483084
(2S,4R)-2-amino-4-[(E)-3-(4-fluorophenyl)prop-2-enyl]pentanedioic acid
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C14H16FNO4
 1
1
Ki = 559 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 = 610 nM
   TI
   LI
   LO
   TS
CP0448648
2-Amino-4-prop-2-ynyl-pentanedioic acid
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C8H11NO4
 1
1
Ki = 823 nM
   TI
   LI
   LO
   TS
CP0394118
2-Amino-4-(3-phenyl-prop-2-ynyl)-pentanedioic acid
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C14H15NO4
 1
1
Ki = 1000 nM
   TI
   LI
   LO
   TS
CP0440472
(2S,4R)-2-amino-4-[(E)-3-(3-chlorophenyl)prop-2-enyl]pentanedioic acid
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C14H16ClNO4
 1
1
Ki = 1132 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 = 1200 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
   Show/Hide
C27H28N6O6
 1
1
Ki = 1400 nM
   TI
   LI
   LO
   TS
CP0479891
(2S,4R)-2-amino-4-[(E)-3-(2-chlorophenyl)prop-2-enyl]pentanedioic acid
   Show/Hide
C14H16ClNO4
 1
1
Ki = 1404 nM
   TI
   LI
   LO
   TS
CP0394121
2-Amino-4-but-2-ynyl-pentanedioic acid
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C9H13NO4
 1
1
Ki = 1456 nM
   TI
   LI
   LO
   TS
CP0358589
2-[7-[3-(aminomethyl)pyrrol-1-yl]-6-nitro-2,3-dioxo-4H-quinoxalin-1-yl]acetic acid
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C15H13N5O6
 1
1
Ki = 1500 nM
   TI
   LI
   LO
   TS
CP0448620
(2S,4R)-2-amino-4-[(E)-3-(2,6-dichlorophenyl)prop-2-enyl]pentanedioic acid
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C14H15Cl2NO4
 1
1
Ki = 1568 nM
   TI
   LI
   LO
   TS
CP0448400
(2S,4R)-2-amino-4-[(E)-3-phenylprop-2-enyl]pentanedioic acid
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C14H17NO4
 1
1
Ki = 1580 nM
   TI
   LI
   LO
   TS
CP0378015
(2S,4R)-4-propylglutamic acid
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C8H15NO4
 1
1
Ki = 2450 nM
   TI
   LI
   LO
   TS
CP0392860
(S)-2-Amino-4-ethylidene-pentanedioic acid
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C7H11NO4
 1
1
Ki = 2500 nM
   TI
   LI
   LO
   TS
CP0521133
2-Amino-4-(3-chloro-allyl)-pentanedioic acid
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C8H12ClNO4
 1
1
Ki = 2893 nM
   TI
   LI
   LO
   TS
CP0429233
2-Amino-4-pent-2-enyl-pentanedioic acid
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C10H17NO4
 1
1
Ki = 2984 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 = 3600 nM
   TI
   LI
   LO
   TS
CP0453300
(2S,4R)-2-amino-4-[(E)-3-(4-nitrophenyl)prop-2-enyl]pentanedioic acid
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C14H16N2O6
 1
1
Ki = 3845 nM
   TI
   LI
   LO
   TS
CP0331934
(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 = 3900 nM
   TI
   LI
   LO
   TS
CP0465001
(2S,4R)-2-amino-4-[(E)-3-(3,4-dichlorophenyl)prop-2-enyl]pentanedioic acid
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C14H15Cl2NO4
 1
1
Ki = 3987 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 = 4100 nM
   TI
   LI
   LO
   TS
CP0451519
(2S,4R)-2-amino-4-[(E)-3-naphthalen-1-ylprop-2-enyl]pentanedioic acid
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C18H19NO4
 1
1
Ki = 4366 nM
   TI
   LI
   LO
   TS
CP0429172
(2S,4R)-2-amino-4-[(E)-3-(4-methylphenyl)prop-2-enyl]pentanedioic acid
   Show/Hide
C15H19NO4
 1
1
Ki = 4375 nM
   TI
   LI
   LO
   TS
CP0441737
(2S,4R)-2-amino-4-[(E)-3-(4-cyanophenyl)prop-2-enyl]pentanedioic acid
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C15H16N2O4
 1
1
Ki = 4491 nM
   TI
   LI
   LO
   TS
CP0395504
2-Amino-4-but-2-enyl-pentanedioic acid
   Show/Hide
C9H15NO4
 1
1
Ki = 5373 nM
   TI
   LI
   LO
   TS
CP0510985
(2S,4R)-2-amino-4-[(E)-3-(4-phenylphenyl)prop-2-enyl]pentanedioic acid
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C20H21NO4
 1
1
Ki = 5650 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
   Show/Hide
C15H10N4O8
 1
1
Ki = 5800 nM
   TI
   LI
   LO
   TS
CP0445213
(2S,4R)-2-amino-4-[(E)-3-(4-methylsulfanylphenyl)prop-2-enyl]pentanedioic acid
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C15H19NO4S
 1
1
Ki = 6024 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 = 6200 nM
   TI
   LI
   LO
   TS
CP0377076
(2S,4R)-2-amino-4-[(E)-3-(3-methoxyphenyl)prop-2-enyl]pentanedioic acid
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C15H19NO5
 1
1
Ki = 6349 nM
   TI
   LI
   LO
   TS
CP0443663
2-Amino-4-hexyl-pentanedioic acid
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C11H21NO4
 1
1
Ki = 7207 nM
   TI
   LI
   LO
   TS
CP0451510
(2S,4R)-2-amino-4-[(E)-3-(4-bromophenyl)prop-2-enyl]pentanedioic acid
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C14H16BrNO4
 1
1
Ki = 7216 nM
   TI
   LI
   LO
   TS
CP0458954
2-Amino-4-(2-chloro-allyl)-pentanedioic acid
   Show/Hide
C8H12ClNO4
 1
1
Ki = 8250 nM
   TI
   LI
   LO
   TS
CP0496520
(2S,4R)-2-Amino-4-(3-phenyl-propyl)-pentanedioic acid
   Show/Hide
C14H19NO4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0493034
(S)-2-Amino-4-[4,4-diphenyl-but-(Z)-ylidene]-pentanedioic acid
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C21H23NO4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0451178
2-Amino-4-pent-2-ynyl-pentanedioic acid
   Show/Hide
C10H15NO4
 1
1
Ki = 10247 nM
   TI
   LI
   LO
   TS
CP0535176
(2S,4R)-2-amino-4-[(E)-3-[4-(trifluoromethoxy)phenyl]prop-2-enyl]pentanedioic acid
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C15H16F3NO5
 1
1
Ki = 11185 nM
   TI
   LI
   LO
   TS
CP0521148
2-Allyl-4-amino-pentanedioic acid
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C8H13NO4
 1
1
Ki = 13800 nM
   TI
   LI
   LO
   TS
CP0496393
(2S,4R)-2-amino-4-[(E)-3-(3,4-dimethoxyphenyl)prop-2-enyl]pentanedioic acid
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C16H21NO6
 1
1
Ki = 13949 nM
   TI
   LI
   LO
   TS
CP0502051
(S)-2-Amino-4-[(E)-but-2-en-(Z)-ylidene]-pentanedioic acid
   Show/Hide
C9H13NO4
 1
1
Ki = 16300 nM
   TI
   LI
   LO
   TS
CP0399917
(S)-2-Amino-4-propylidene-pentanedioicacid
   Show/Hide
C8H13NO4
 1
1
Ki = 18000 nM
   TI
   LI
   LO
   TS
CP0515816
(2S,4R)-2-amino-4-[(E)-3-(4-methoxyphenyl)prop-2-enyl]pentanedioic acid
   Show/Hide
C15H19NO5
 1
1
Ki = 22340 nM
   TI
   LI
   LO
   TS
CP0873915
2-Amino-4-pent-2-enyl-pentanedioic acid
   Show/Hide
C10H17NO4
 1
1
Ki = 22529 nM
   TI
   LI
   LO
   TS
CP0398226
3-(7-{3-[(Benzyl-methyl-amino)-methyl]-pyrrol-1-yl}-6-nitro-2,3-dioxo-3,4-dihydro-2H-quinoxalin-1-yl)-propionic acid
   Show/Hide
C24H23N5O6
 1
1
Ki = 23000 nM
   TI
   LI
   LO
   TS
CP0501243
(2S,4R)-2-amino-4-[(E)-3-(4-carboxyphenyl)prop-2-enyl]pentanedioic acid
   Show/Hide
C15H17NO6
 1
1
Ki = 27280 nM
   TI
   LI
   LO
   TS
CP0429157
(2S,4R)-2-amino-4-[(E)-3-(4-propan-2-ylphenyl)prop-2-enyl]pentanedioic acid
   Show/Hide
C17H23NO4
 1
1
Ki = 27532 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
   Show/Hide
C20H21N5O6
 1
1
Ki = 28000 nM
   TI
   LI
   LO
   TS
CP0378229
(2S,4R)-4-pentylglutamic acid
   Show/Hide
C10H19NO4
 1
1
Ki = 41152 nM
   TI
   LI
   LO
   TS
CP0448863
2-Amino-4-(3-methyl-but-2-enyl)-pentanedioic acid
   Show/Hide
C10H17NO4
 1
1
Ki = 42809 nM
   TI
   LI
   LO
   TS
CP0397870
(2S,4R)-2-amino-4-[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enyl]pentanedioic acid
   Show/Hide
C15H16F3NO4
 1
1
Ki = 43929 nM
   TI
   LI
   LO
   TS
CP0501493
(S)-2-Amino-4-[2,2-dimethyl-cyclopent-(Z)-ylidene]-pentanedioic acid
   Show/Hide
C12H19NO4
 1
1
Ki = 46300 nM
   TI
   LI
   LO
   TS
CP0508637
(S)-2-Amino-4-butylidene-pentanedioic acid
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C9H15NO4
 1
1
Ki = 57200 nM
   TI
   LI
   LO
   TS
CP0429234
2-Amino-4-hex-2-ynyl-pentanedioic acid
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C11H17NO4
 1
1
Ki = 68547 nM
   TI
   LI
   LO
   TS
CP0376766
(2S,4E)-2-amino-4-(2-methylpropylidene)pentanedioic acid
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C9H15NO4
 1
1
Ki = 82500 nM
   TI
   LI
   LO
   TS
CP0391361
(S)-2-Amino-4-[1-cyclopentyl-meth-(E)-ylidene]-pentanedioic acid
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C11H17NO4
 1
1
Ki = 87600 nM
   TI
   LI
   LO
   TS
CP0403533
(S)-2-Amino-4-[(E)-3-phenyl-prop-2-en-(E)-ylidene]-pentanedioic acid
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C14H15NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0448006
(S)-2-Amino-4-(2,2-dimethyl-propylidene)-pentanedioic acid
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C10H17NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0488123
(S)-2-Amino-4-cyclobutylidene-pentanedioic acid
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C9H13NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0497639
(S)-2-Amino-4-[2,2-dimethyl-cyclopent-(E)-ylidene]-pentanedioic acid
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C12H19NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0502379
(S)-2-Amino-4-[4,4-diphenyl-but-(E)-ylidene]-pentanedioic acid
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C21H23NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0067501
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
 1
1 EC50 > 100000 nM
CP0000105
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid
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C10H15NO4
 1
1 Ki = 53 nM
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 1
1 Ki = 1106 nM
CP0008315
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
 1
1 Ki = 13200 nM
CP0067480
(3S,4aR,6R,8aR)-6-[2-(2H-tetrazol-5-yl)ethyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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C13H21N5O2
 1
1 Ki > 100000 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic kainate 2 (GRIK2) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02201 Glutamate receptor ionotropic, kainate 2 Rattus norvegicus, Rat