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TargetGlutamate receptor 2
LigandBDBM50599760
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2231632 (CHEMBL5145404)
IC50 22000±n/a nM
Citation Sakurai, FYukawa, TKina, AMurakami, MTakami, KMorimoto, SSeto, MKamata, MYamashita, TNakashima, KNarita, NBettini, EUgolini, ACorsi, MHasui, T Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity. Bioorg Med Chem56:0 (2022) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glutamate receptor 2
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:
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50599760
n/a
NameBDBM50599760
Synonyms:CHEMBL5194021
TypeSmall organic molecule
Emp. Form.C19H20FN5O
Mol. Mass.353.3934
SMILESCCN(Cc1cc2n(n1)c(C)cn(CCC#N)c2=O)c1ccc(F)cc1
Structure
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