General Information of the Protein
Protein ID
PT01518
Protein Name
Glutamate receptor ionotropic, kainate 1
Secondarily
Protein Name
Excitatory amino acid receptor 3
Glutamate receptor 5
Gene Name
GRIK1
Secondarily
Gene Name
GLUR5
Sequence
MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKFAVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQSICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDSTGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEILKQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSMERLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRFMNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGIWNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCLDLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFTPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKMWAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYGVGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFIVLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECGKLIREERGIRKQSSVHTV
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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. May be involved in the transmission of light information from the retina to the hypothalamus.
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Uniprot ID
Primary ID:
P39086

Secondarily ID:
Q13001
Q86SU9
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Ensembl ID
ENSG00000171189
HGNC ID
HGNC:4579
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: CL000026 , CHO-K1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0433434
 Compound Info 
(S)-1-(2'-Amino-2'-carboxyethyl)thieno[3,2-d]pyrimidin-2,4-dione
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C9H9N3O4S
  1
1
IC50 = 1.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0376771
 Compound Info 
(S)-1-[2'-Amino-2'-carboxyethyl]-5,7-dihydrothieno[3,4-d]pyrimidin-2,4(1H,3H)-dione
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C9H11N3O4S
  1
1
IC50 = 3.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0067501
 Compound Info 
(2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid
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C18H19NO4
  1
1 EC50 = 2500 nM
CP0162369
 Compound Info 
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid
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C14H10BrClN2O3
  1
1 IC50 > 30000 nM
CP0374730
 Compound Info 
4-Chloro-2-(3-naphthalen-2-yl-ureido)-benzoic acid
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C18H13ClN2O3
  1
1 IC50 > 30000 nM
CP0051516
 Compound Info 
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
CP0312285
 Compound Info 
2-[3-(3-bromophenyl)ureido]-4-chlorobenzenesulfonic acid
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C13H10BrClN2O4S
  1
1 IC50 > 30000 nM
CP0346386
 Compound Info 
2-[2-[(3-bromophenyl)carbamoylamino]-4-chlorophenyl]acetic acid
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C15H12BrClN2O3
  1
1 IC50 > 30000 nM
CP0378727
 Compound Info 
1-(3-bromophenyl)-3-[5-chloro-2-(1H-tetrazol-5-yl-phenyl]urea
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C14H10BrClN6O
  1
1 IC50 > 30000 nM
CP0008315
 Compound Info 
2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide
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C12H8N4O6S
  1
1 Ki = 11730 nM
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic kainate 1 (GRIK1) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Alcohol dependence [ICD-11: 6C40.2]
2 Pain [ICD-11: MG30-MG3Z]
3 Neuropathic pain [ICD-11: 8E43.0]
4 Neurological disorder [ICD-11: 6B60]
Approved Drug(s) 1 Approved Drug  1
1 Topiramate
 Drug Info 
Approved
Alcohol dependence
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 LY293558
 Drug Info 
Phase 2
Pain
2 NS 1209
 Drug Info 
Phase 2
Neuropathic pain
3 NBQX
 Drug Info 
Phase 1
Neurological disorder
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02200 Glutamate receptor ionotropic, kainate 1 Rattus norvegicus, Rat
 Protein Info