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Target
Glutamate receptor 2
Ligand
BDBM50205852
Substrate
n/a
Meas. Tech.
ChEMBL_1628579 (CHEMBL3871164)
EC50
210±n/a nM
Citation
 Villemure, E; Volgraf, M; Jiang, Y; Wu, G; Ly, CQ; Yuen, PW; Lu, A; Luo, X; Liu, M; Zhang, S; Lupardus, PJ; Wallweber, HJ; Liederer, BM; Deshmukh, G; Plise, E; Tay, S; Wang, TM; Hanson, JE; Hackos, DH; Scearce-Levie, K; Schwarz, JB; Sellers, BD GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved ACS Med Chem Lett 8:84-89 (2017) [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:
BDBM50205852
Synonyms:
CHEMBL3976578 | US10280165, Example 38
Type:
Small organic molecule
Emp. Form.:
C18H13ClF3N5O
Mol. Mass.:
407.777
SMILES:
Cc1cc([C@@H]2C[C@H]2C#N)n2c(c1)nc(Cn1nc(cc1Cl)C(F)(F)F)cc2=O |r|
Structure:
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