Reaction Details |
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Target | Glutamate receptor 1 |
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Ligand | BDBM50105843 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_878020 (CHEMBL2182446) |
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IC50 | 65±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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BDBM50105843 |
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n/a |
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Name | BDBM50105843 |
Synonyms: | 2-Amino-N-{3-[4-(3-amino-propylamino)-butylamino]-propyl}-acetamide | CHEMBL313747 | Joro spider toxin 3 | N*1*-(5-{3-[4-(3-Amino-propylamino)-butylamino]-propionylamino}-pentyl)-2-[2-(2,4-dihydroxy-phenyl)-acetylamino]-succinamide |
Type | Small organic molecule |
Emp. Form. | C27H47N7O6 |
Mol. Mass. | 565.7054 |
SMILES | NCCCNCCCCNCCC(=O)NCCCCCNC(=O)[C@H](CC(N)=O)NC(=O)Cc1ccc(O)cc1O |
Structure |
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