Reaction Details Report a problem with these data
Target
Glutamate receptor 2
Ligand
BDBM50191959
Substrate
n/a
Meas. Tech.
ChEMBL_391778 (CHEMBL871565)
EC50
309±n/a nM
Citation
Fernandez, MC; Castaño, A; Dominguez, E; Escribano, A; Jiang, D; Jimenez, A; Hong, E; Hornback, WJ; Nisenbaum, ES; Rankl, N; Tromiczak, E; Vaught, G; Zarrinmayeh, H; Zimmerman, DM A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives. Bioorg Med Chem Lett 16:5057-61 (2006) [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:
BDBM50191959
Synonyms:
3-(4-tert-butylphenyl)-4-cyano-5-(methylthio)thiophene-2-carboxylic acid | 3-(4-tert-butylphenyl)-4-cyano-5-methylsulfanyl-thiophene-2-carboxylic acid | CHEMBL213197
Type:
Small organic molecule
Emp. Form.:
C17H17NO2S2
Mol. Mass.:
331.452
SMILES:
CSc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C