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Target
Glutamate receptor 1
Ligand
BDBM50184414
Substrate
n/a
Meas. Tech.
ChEMBL_1586963 (CHEMBL3825097)
IC50
>83300±n/a nM
Citation
 Gardinier, KM; Gernert, DL; Porter, WJ; Reel, JK; Ornstein, PL; Spinazze, P; Stevens, FC; Hahn, P; Hollinshead, SP; Mayhugh, D; Schkeryantz, J; Khilevich, A; De Frutos, O; Gleason, SD; Kato, AS; Luffer-Atlas, D; Desai, PV; Swanson, S; Burris, KD; Ding, C; Heinz, BA; Need, AB; Barth, VN; Stephenson, GA; Diseroad, BA; Woods, TA; Yu, H; Bredt, D; Witkin, 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:
BDBM50184414
Synonyms:
CHEMBL3823131
Type:
Small organic molecule
Emp. Form.:
C16H12N4OS2
Mol. Mass.:
340.423
SMILES:
CN(c1nc(cs1)-c1ccccn1)c1ccc2[nH]c(=O)sc2c1
Structure:
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