Reaction Details  Report a problem with these data
Target
Glutamate receptor 1
Ligand
BDBM50105843
Substrate
n/a
Meas. Tech.
ChEMBL_878020 (CHEMBL2182446)
IC50
65±n/a nM
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 Chem 55:10297-301 (2012) [PubMed]  Article
Target
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:
MPYIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQEALISIIDHYKWQTFVYIYDADRGLSVLQRVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIVKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPARIMQQWRTSDSRDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASGGGGSGENGRVVSQDFPKSMQSIPCMSHSSGMPLGATGL
  
Inhibitor
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:
Search PDB for entries with ligand similarity: