Reaction Details Report a problem with these data
Target
Glutamate receptor 2
Ligand
BDBM50251235
Substrate
n/a
Meas. Tech.
ChEMBL_1683301 (CHEMBL4033578)
EC50
450±n/a nM
Citation
 Goffin, E; Drapier, T; Larsen, AP; Geubelle, P; Ptak, CP; Laulumaa, S; Rovinskaja, K; Gilissen, J; Tullio, P; Olsen, L; Frydenvang, K; Pirotte, B; Hanson, J; Oswald, RE; Kastrup, JS; Francotte, P 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of?-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. J Med Chem 61:251-264 (2018) [PubMed]  Article 
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:
BDBM50251235
Synonyms:
CHEMBL4066717
Type:
Small organic molecule
Emp. Form.:
C17H15N3O3S
Mol. Mass.:
341.384
SMILES:
O=S1(=O)NCN(C2CC2)c2ccc(Oc3cccc(c3)C#N)cc12
Structure:
Search PDB for entries with ligand similarity: