Reaction Details |
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Target | Glutamate receptor ionotropic, kainate 1 |
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Ligand | BDBM50207594 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_303286 (CHEMBL828279) |
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Ki | 11730±n/a nM |
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Citation | Dominguez, E; Iyengar, S; Shannon, HE; Bleakman, D; Alt, A; Arnold, BM; Bell, MG; Bleisch, TJ; Buckmaster, JL; Castano, AM; Del Prado, M; Escribano, A; Filla, SA; Ho, KH; Hudziak, KJ; Jones, CK; Martinez-Perez, JA; Mateo, A; Mathes, BM; Mattiuz, EL; Ogden, AM; Simmons, RM; Stack, DR; Stratford, RE; Winter, MA; Wu, Z; Ornstein, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Glutamate receptor ionotropic, kainate 1 |
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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
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BDBM50207594 |
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n/a |
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Name | BDBM50207594 |
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 |
Type | Small organic molecule |
Emp. Form. | C12H8N4O6S |
Mol. Mass. | 336.28 |
SMILES | NS(=O)(=O)c1cccc2c1c(cc1[nH]c(=O)c(=O)[nH]c21)[N+]([O-])=O |
Structure |
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