| Reaction Details |
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 | Report a problem with these data |
| Target | Glutamate receptor 2 |
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| Ligand | BDBM50164444 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1574110 (CHEMBL3801520) |
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| EC50 | 359±n/a nM |
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| Citation |  Volgraf, M; Sellers, BD; Jiang, Y; Wu, G; Ly, CQ; Villemure, E; Pastor, RM; Yuen, PW; Lu, A; Luo, X; Liu, M; Zhang, S; Sun, L; Fu, Y; Lupardus, PJ; Wallweber, HJ; Liederer, BM; Deshmukh, G; Plise, E; Tay, S; Reynen, P; Herrington, J; Gustafson, A; Liu, Y; Dirksen, A; Dietz, MG; Liu, Y; Wang, TM; Hanson, JE; Hackos, D; Scearce-Levie, K; Schwarz, JB Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design. J Med Chem59:2760-79 (2016) [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 |
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| 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 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 98825.96 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Glutamate AMPA 2 GRIA2 HUMAN::P42262 |
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| Residue: | 883 |
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| Sequence: | MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
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| BDBM50164444 |
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| n/a |
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| Name | BDBM50164444 |
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| Synonyms: | CHEMBL3800605 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H16F4N2O2S |
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| Mol. Mass. | 412.401 |
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| SMILES | Cc1sc2nc(Cc3cccc(c3F)C(F)(F)F)cc(=O)n2c1C1CC1CO |
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| Structure | 
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