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Target
Glutamate receptor ionotropic, kainate 2
Ligand
BDBM50207594
Substrate
n/a
Meas. Tech.
ChEMBL_90593 (CHEMBL701338)
Ki
13200±n/a nM
Citation
Filla, SA; Winter, MA; Johnson, KW; Bleakman, D; Bell, MG; Bleisch, TJ; Castaño, AM; Clemens-Smith, A; del Prado, M; Dieckman, DK; Dominguez, E; Escribano, A; Ho, KH; Hudziak, KJ; Katofiasc, MA; Martinez-Perez, JA; Mateo, A; Mathes, BM; Mattiuz, EL; Ogden, AM; Phebus, LA; Stack, DR; Stratford, RE; Ornstein, PL Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. J Med Chem 45:4383-6 (2002) [PubMed] Article
More Info.:
Target
Name:
Glutamate receptor ionotropic, kainate 2
Synonyms:
EAA4 | Excitatory amino acid receptor 4 | GLUR6 | GRIK2 | GRIK2_HUMAN | GluK2 | GluR-6 | Glutamate kainate | Glutamate receptor 6 | Glutamate receptor ionotropic kainate 2 | Glutamate receptor, ionotropic kainate 2 | Glutamate-Kainate | Glutamate-Kainate, GluR6
Type:
Enzyme Catalytic Domain
Mol. Mass.:
102592.78
Organism:
Homo sapiens (Human)
Description:
Q13002
Residue:
908
Sequence:
MKIIFPILSNPVFRRTVKLLLCLLWIGYSQGTTHVLRFGGIFEYVESGPMGAEELAFRFAVNTINRNRTLLPNTTLTYDTQKINLYDSFEASKKACDQLSLGVAAIFGPSHSSSANAVQSICNALGVPHIQTRWKHQVSDNKDSFYVSLYPDFSSLSRAILDLVQFFKWKTVTVVYDDSTGLIRLQELIKAPSRYNLRLKIRQLPADTKDAKPLLKEMKRGKEFHVIFDCSHEMAAGILKQALAMGMMTEYYHYIFTTLDLFALDVEPYRYSGVNMTGFRILNTENTQVSSIIEKWSMERLQAPPKPDSGLLDGFMTTDAALMYDAVHVVSVAVQQFPQMTVSSLQCNRHKPWRFGTRFMSLIKEAHWEGLTGRITFNKTNGLRTDFDLDVISLKEEGLEKIGTWDPASGLNMTESQKGKPANITDSLSNRSLIVTTILEEPYVLFKKSDKPLYGNDRFEGYCIDLLRELSTILGFTYEIRLVEDGKYGAQDDANGQWNGMVRELIDHKADLAVAPLAITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYILLAYLGVSCVLFVIARFSPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVEDGATMTFFKKSKISTYDKMWAFMSSRRQSVLVKSNEEGIQRVLTSDYAFLMESTTIEFVTQRNCNLTQIGGLIDSKGYGVGTPMGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEESKEASALGVQNIGGIFIVLAAGLVLSVFVAVGEFLYKSKKNAQLEKRSFCSAMVEELRMSLKCQRRLKHKPQAPVIVKTEEVINMHTFNDRRLPGKETMA
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