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TargetGlutamate receptor ionotropic, kainate 1
LigandBDBM50207594
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303286 (CHEMBL828279)
Ki 11730±n/a nM
Citation Dominguez, EIyengar, SShannon, HEBleakman, DAlt, AArnold, BMBell, MGBleisch, TJBuckmaster, JLCastano, AMDel Prado, MEscribano, AFilla, SAHo, KHHudziak, KJJones, CKMartinez-Perez, JAMateo, AMathes, BMMattiuz, ELOgden, AMSimmons, RMStack, DRStratford, REWinter, MAWu, ZOrnstein, PL Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem48:4200-3 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glutamate receptor ionotropic, kainate 1
Name:Glutamate receptor ionotropic, kainate 1
Synonyms:GLUR5 | GRIK1 | GRIK1_HUMAN | Glutamate Receptor | Glutamate kainate | Glutamate receptor ionotropic kainate | Glutamate receptor ionotropic kainate 1 | Glutamate receptor, ionotropic kainate 1 | Glutamate-Kainate | Glutamate-Kainate, GluR5 | Grik1 protein | hmglur5 flipr
Type:Enzyme Catalytic Domain
Mol. Mass.:103984.96
Organism:Homo sapiens (Human)
Description:P39086
Residue:918
Sequence:
MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKF
AVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQ
SICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDS
TGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEIL
KQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSME
RLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRF
MNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGI
WNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCL
DLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREK
VIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFT
PYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTL
IIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKM
WAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYG
VGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFI
VLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECG
KLIREERGIRKQSSVHTV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50207594
n/a
NameBDBM50207594
Synonyms:2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfonic acid amide | 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline | 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline | 3-Hydroxy-6-nitro-7-sulfamoyl-benzo[f]quinoxalin-2-ol anion | 6-Nitro-2,3-dioxo-1,2,3,4,4a,10b-hexahydro-benzo[f]quinoxaline-7-sulfonic acid amide | 6-Nitro-2,3-dioxo-1,2,3,4-tetrahydro-benzo[f]quinoxaline-7-sulfinic acid amide | 6-Nitro-2,3-dioxo-1,2,3,4-tetrahydro-benzo[f]quinoxaline-7-sulfonic acid amide | 6-Nitro-2,3-dioxo-2,3-dihydro-benzo[f]quinoxaline-7-sulfonic acid amide | 6-nitro-2,3-dioxo-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide | CHEMBL222519
TypeSmall organic molecule
Emp. Form.C12H8N4O6S
Mol. Mass.336.28
SMILESNS(=O)(=O)c1cccc2c1c(cc1[nH]c(=O)c(=O)[nH]c21)[N+]([O-])=O
Structure
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