Reaction Details Report a problem with these data
Target
Glutamate receptor 2
Ligand
BDBM50207593
Substrate
n/a
Meas. Tech.
ChEMBL_429155 (CHEMBL914410)
IC50
>100000±n/a nM
Citation
Dolman, NP; More, JC; Alt, A; Knauss, JL; Pentikäinen, OT; Glasser, CR; Bleakman, D; Mayer, ML; Collingridge, GL; Jane, DE Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J Med Chem 50:1558-70 (2007) [PubMed] Article
More Info.:
Target
Name:
Glutamate receptor 2
Synonyms:
AMPA-selective glutamate receptor 2 | GLUR2 | GRIA2 | GRIA2_HUMAN | GluR-2 | GluR-B | GluR-K2 | Glutamate AMPA 2 | Glutamate receptor 2 | Glutamate receptor AMPA 1/2 | Glutamate receptor AMPA 2/3 | Glutamate receptor ionotropic AMPA | Glutamate receptor ionotropic, AMPA 2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
98825.96
Organism:
Homo sapiens (Human)
Description:
Glutamate AMPA 2 GRIA2 HUMAN::P42262
Residue:
883
Sequence:
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTPHIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDGTHPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINVGNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANLGFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALTYDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNIKFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTTILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKIWNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLSKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSRAEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Inhibitor
Name:
BDBM50207593
Synonyms:
(S)-1-(2-AMINO-2-CARBOXYETHYL)-3(2-CARBOXYTHIOPHENE-3-YL-METHYL)-5-METHYLPYRIMIDINE-2,4-DIONE | (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxythiophene-3-ylmethyl)-5-methylpyrimidine-2,4-dione | CHEMBL373428
Type:
Small organic molecule
Emp. Form.:
C14H15N3O6S
Mol. Mass.:
353.35
SMILES:
Cc1cn(C[C@H](N)C(O)=O)c(=O)n(Cc2ccsc2C(O)=O)c1=O