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Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50168965
Substrate
n/a
Meas. Tech.
ChEMBL_303286 (CHEMBL828279)
Ki
1690±n/a nM
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 Chem 48:4200-3 (2005) [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:
BDBM50168965
Synonyms:
(3S,4aS,6S,8aR)-6-[2-(1H-Tetrazol-5-yl)-phenoxy]-decahydro-isoquinoline-3-carboxylic acid | CHEMBL189985
Type:
Small organic molecule
Emp. Form.:
C17H21N5O3
Mol. Mass.:
343.3803
SMILES:
OC(=O)[C@@H]1C[C@H]2C[C@H](CC[C@H]2CN1)Oc1ccccc1-c1nnn[nH]1
Structure:
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