Reaction Details |
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Target | Glutamate receptor 2 |
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Ligand | BDBM50192217 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_391777 (CHEMBL871564) |
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EC50 | 1137±n/a nM |
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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 Lett16:5057-61 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glutamate receptor 2 |
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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
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BDBM50192217 |
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n/a |
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Name | BDBM50192217 |
Synonyms: | 3-(4-tert-butylphenyl)-4-cyano-5-(pyrrolidin-1-yl)thiophene-2-carboxylic acid | CHEMBL387304 |
Type | Small organic molecule |
Emp. Form. | C20H22N2O2S |
Mol. Mass. | 354.466 |
SMILES | CC(C)(C)c1ccc(cc1)-c1c(sc(N2CCCC2)c1C#N)C(O)=O |
Structure |
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