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TargetGRIA1
LigandBDBM50184410
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1586961
IC50 243±n/a nM
Citation Gardinier, KMGernert, DLPorter, WJReel, JKOrnstein, PLSpinazze, PStevens, FCHahn, PHollinshead, SPMayhugh, DSchkeryantz, JKhilevich, ADe Frutos, OGleason, SDKato, ASLuffer-Atlas, DDesai, PVSwanson, SBurris, KDDing, CHeinz, BANeed, ABBarth, VNStephenson, GADiseroad, BAWoods, TAYu, HBredt, DWitkin, JM Discovery of the Firsta-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP)-8. J Med Chem59:4753-68 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
GRIA1
Name:Glutamate receptor AMPA 1/2
Synonyms:AMPA-selective glutamate receptor 1 | GluR-1 | GluR-A | GluR-K1 | Glutamate AMPA 1 | Glutamate receptor 1 | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50184410
NameBDBM50184410
Synonyms:CHEBI:71013 | E-2007 | E2007 | ER-155055-90 | Fycompa | PERAMPANEL | Perampanel
TypeSmall organic molecule
Emp. Form.C23H15N3O
Mol. Mass.349.3847
SMILESO=c1c(cc(cn1-c1ccccc1)-c1ccccn1)-c1ccccc1C#N
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a