Target
Glutamate receptor 1
Ligand
BDBM426142
Substrate
n/a
Meas. Tech.
Calcium Flux Assay
IC50
0.400±n/a nM
Citation
 Ameriks, MKSavall, BMSwanson, DMWu, D Imidazopyrazines and pyrazolopyrimidines and their use as AMPA receptor modulators US Patent  US10513523 Publication Date 12/24/2019 
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:
BDBM426142
Synonyms:
5-[8-(3-Fluoroazetidin-1-yl)-2-phenyl-imidazo[1,2-a]pyrazin-3-yl]indolin- | US10513523, Example 81
Type:
Small organic molecule
Emp. Form.:
C23H18FN5O
Mol. Mass.:
399.4203
SMILES:
FC1CN(C1)c1nccn2c(c(nc12)-c1ccccc1)-c1ccc2NC(=O)Cc2c1
Structure:
Search PDB for entries with ligand similarity: