Reaction Details |
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Target | Glutamate receptor 1 |
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Ligand | BDBM50316373 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_878020 (CHEMBL2182446) |
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IC50 | 135±n/a nM |
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Citation | Lucas, S; Poulsen, MH; Nørager, NG; Barslund, AF; Bach, TB; Kristensen, AS; Strømgaard, K General synthesis ofß-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. J Med Chem55:10297-301 (2012) [PubMed] Article |
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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 | GRIA1_RAT | GluA1 | GluR-1 | GluR-A | GluR-K1 | Glur1 | Glutamate receptor ionotropic, AMPA 1 | Gria1 |
Type: | Protein |
Mol. Mass.: | 101583.91 |
Organism: | Rattus norvegicus (Rat) |
Description: | P19490 |
Residue: | 907 |
Sequence: | MPYIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQID
IVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQ
FVLQLRPELQEALISIIDHYKWQTFVYIYDADRGLSVLQRVLDTAAEKNWQVTAVNILTT
TEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIVKLEKNGIGYHYILANLGFMDIDL
NKFKESGANVTGFQLVNYTDTIPARIMQQWRTSDSRDHTRVDWKRPKYTSALTYDGVKVM
AEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGR
RTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV
MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGE
LVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIW
MCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQ
QGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIA
YGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLES
TMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKW
WYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK
GFCLIPQQSINEAIRTSTLPRNSGAGASGGGGSGENGRVVSQDFPKSMQSIPCMSHSSGM
PLGATGL
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BDBM50316373 |
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n/a |
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Name | BDBM50316373 |
Synonyms: | Argiotoxin-636 | CHEMBL1098240 |
Type | Small organic molecule |
Emp. Form. | C29H52N10O6 |
Mol. Mass. | 636.7866 |
SMILES | [#7]-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#7]-[#6]-[#6]-[#6]-[#7]-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6@H](-[#6]-[#6](-[#7])=O)-[#7]-[#6](=O)-[#6]-c1ccc(-[#8])cc1-[#8] |r| |
Structure |
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