Target
Glutamate receptor 1
Ligand
BDBM50184441
Substrate
n/a
Meas. Tech.
ChEMBL_1586960 (CHEMBL3825094)
IC50
9260±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 Chem 59:4753-68 (2016) [PubMed]  Article 
Target
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:
MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMPLGATGL
  
Inhibitor
Name:
BDBM50184441
Synonyms:
CHEMBL3823817
Type:
Small organic molecule
Emp. Form.:
C22H24N4O2S
Mol. Mass.:
408.517
SMILES:
C[C@H](c1ccn(n1)-c1ccc(CCC(C)(C)O)cn1)c1ccc2[nH]c(=O)sc2c1 |r|
Structure:
Search PDB for entries with ligand similarity: