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Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50207594
Substrate
n/a
Meas. Tech.
ChEMBL_429156 (CHEMBL914411)
IC50
37000±n/a nM
Citation
 Dolman, NP; More, JC; Alt, A; Knauss, JL; Pentikäinen, OT; Glasser, CR; Bleakman, D; Mayer, ML; Collingridge, GL; Jane, DE Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J Med Chem 50:1558-70 (2007) [PubMed]  Article 
Target
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:
MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKFAVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQSICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDSTGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEILKQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSMERLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRFMNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGIWNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCLDLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFTPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKMWAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYGVGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFIVLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECGKLIREERGIRKQSSVHTV
  
Inhibitor
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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