Reaction Details |
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Target | Glutamate receptor 2 |
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Ligand | BDBM50494067 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_990075 (CHEMBL2443752) |
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Ki | 3300±n/a nM |
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Citation | Martinez-Perez, JA; Iyengar, S; Shannon, HE; Bleakman, D; Alt, A; Arnold, BM; Bell, MG; Bleisch, TJ; Castaņo, AM; Del Prado, M; Dominguez, E; Escribano, AM; Filla, SA; Ho, KH; Hudziak, KJ; Jones, CK; Mateo, A; Mathes, BM; Mattiuz, EL; Ogden, AM; Simmons, RM; Stack, DR; Stratford, RE; Winter, MA; Wu, Z; Ornstein, PL GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models. Bioorg Med Chem Lett23:6459-62 (2013) [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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BDBM50494067 |
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n/a |
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Name | BDBM50494067 |
Synonyms: | CHEMBL2440517 |
Type | Small organic molecule |
Emp. Form. | C17H21ClN2O4 |
Mol. Mass. | 352.813 |
SMILES | [H][C@@]12CC[C@@H](C[C@]1([H])C[C@H](NC2)C(O)=O)Nc1ccc(Cl)cc1C(O)=O |r| |
Structure |
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