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Target
Glutamate receptor ionotropic, kainate 5
Ligand
BDBM50168962
Substrate
n/a
Ki
4000±n/a nM
Comments
PDSP_6661
Citation
Weiss, B; Alt, A; Ogden, AM; Gates, M; Dieckman, DK; Clemens-Smith, A; Ho, KH; Jarvie, K; Rizkalla, G; Wright, RA; Calligaro, DO; Schoepp, D; Mattiuz, EL; Stratford, RE; Johnson, B; Salhoff, C; Katofiasc, M; Phebus, LA; Schenck, K; Cohen, M; Filla, SA; Ornstein, PL; Johnson, KW; Bleakman, D Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo. J Pharmacol Exp Ther 318:772-81 (2006) [PubMed] Article
More Info.:
Target
Name:
Glutamate receptor ionotropic, kainate 5
Synonyms:
GRIK2 | GRIK5 | GRIK5_HUMAN | Glutamate receptor ionotropic kainate 5 | Glutamate receptor, ionotropic kainate 5 | Glutamate-Kainate 5 | Ionotropic glutamate receptor kainate 2/5
Type:
Enzyme Catalytic Domain
Mol. Mass.:
109280.81
Organism:
Homo sapiens (Human)
Description:
Glutamate-Kainate 5 Grik5 HUMAN::Q16478
Residue:
980
Sequence:
MPAELLLLLIVAFASPSCQVLSSLRMAAILDDQTVCGRGERLALALAREQINGIIEVPAKARVEVDIFELQRDSQYETTDTMCQILPKGVVSVLGPSSSPASASTVSHICGEKEIPHIKVGPEETPRLQYLRFASVSLYPSNEDVSLAVSRILKSFNYPSASLICAKAECLLRLEELVRGFLISKETLSVRMLDDSRDPTPLLKEIRDDKVSTIIIDANASISHLILRKASELGMTSAFYKYILTTMDFPILHLDGIVEDSSNILGFSMFNTSHPFYPEFVRSLNMSWRENCEASTYLGPALSAALMFDAVHVVVSAVRELNRSQEIGVKPLACTSANIWPHGTSLMNYLRMVEYDGLTGRVEFNSKGQRTNYTLRILEKSRQGHREIGVWYSNRTLAMNATTLDINLSQTLANKTLVVTTILENPYVMRRPNFQALSGNERFEGFCVDMLRELAELLRFRYRLRLVEDGLYGAPEPNGSWTGMVGELINRKADLAVAAFTITAEREKVIDFSKPFMTLGISILYRVHMGRKPGYFSFLDPFSPAVWLFMLLAYLAVSCVLFLAARLSPYEWYNPHPCLRARPHILENQYTLGNSLWFPVGGFMQQGSEIMPRALSTRCVSGVWWAFTLIIISSYTANLAAFLTVQRMEVPVESADDLADQTNIEYGTIHAGSTMTFFQNSRYQTYQRMWNYMQSKQPSVFVKSTEEGIARVLNSRYAFLLESTMNEYHRRLNCNLTQIGGLLDTKGYGIGMPLGSPFRDEITLAILQLQENNRLEILKRKWWEGGRCPKEEDHRAKGLGMENIGGIFIVLICGLIIAVFVAVMEFIWSTRRSAESEEVSVCQEMLQELRHAVSCRKTSRSRRRRRPGGPSRALLSLRAVREMRLSNGKLYSAGAGGDAGSAHGGPQRLLDDPGPPSGARPAAPTPCTHVRVCQECRRIQALRASGAGAPPRGLGVPAEATSPPRPRPGPAGPRELAEHE
Inhibitor
Name:
BDBM50168962
Synonyms:
(3S,4aR,6S,8aR)-6-(4-Carboxy-benzyl)-decahydro-isoquinoline-3-carboxylic acid | 6-(4-Carboxy-benzyl)-decahydro-isoquinoline-3-carboxylic acid | CHEMBL274226 | LY 382884
Type:
Small organic molecule
Emp. Form.:
C18H23NO4
Mol. Mass.:
317.3795
SMILES:
OC(=O)[C@@H]1C[C@H]2C[C@@H](Cc3ccc(cc3)C(O)=O)CC[C@H]2CN1