Reaction Details |
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Target | Glutamate receptor 1 |
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Ligand | BDBM86751 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_90140 (CHEMBL701239) |
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Ki | 9200±n/a nM |
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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 Chem45:4383-6 (2002) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Glutamate receptor 1 |
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Name: | Glutamate receptor 1 |
Synonyms: | AMPA-selective glutamate receptor 1 | GLUH1 | GLUR1 | GRIA1 | GRIA1_HUMAN | GluR-1 | GluR-A | GluR-K1 | Glutamate AMPA 1 | Glutamate receptor 1 | Glutamate receptor AMPA 1/2 | Glutamate receptor ionotropic AMPA | Glutamate receptor ionotropic, AMPA 1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 101512.92 |
Organism: | Homo sapiens (Human) |
Description: | Glutamate AMPA 1 GRIA1 HUMAN::P42261 |
Residue: | 906 |
Sequence: | MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQID
IVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQ
FVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTT
TEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDL
NKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVM
AEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGR
RTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV
MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGE
LVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIW
MCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQ
QGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIA
YGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLES
TMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKW
WYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK
GFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMP
LGATGL
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BDBM86751 |
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n/a |
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Name | BDBM86751 |
Synonyms: | CHEMBL14935 | LY 293558 | LY-293558 |
Type | Small organic molecule |
Emp. Form. | C13H21N5O2 |
Mol. Mass. | 279.3381 |
SMILES | OC(=O)[C@@H]1C[C@H]2C[C@@H](CCc3nnn[nH]3)CC[C@H]2CN1 |
Structure |
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