| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 8 |
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| Ligand | BDBM50558766 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2064719 (CHEMBL4719972) |
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| EC50 | 1770±n/a nM |
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| Citation |  Chappell, MD; Li, R; Smith, SC; Dressman, BA; Tromiczak, EG; Tripp, AE; Blanco, MJ; Vetman, T; Quimby, SJ; Matt, J; Britton, TC; Fivush, AM; Schkeryantz, JM; Mayhugh, D; Erickson, JA; Bures, MG; Jaramillo, C; Carpintero, M; Diego, JE; Barberis, M; Garcia-Cerrada, S; Soriano, JF; Antonysamy, S; Atwell, S; MacEwan, I; Condon, B; Sougias, C; Wang, J; Zhang, A; Conners, K; Groshong, C; Wasserman, SR; Koss, JW; Witkin, JM; Li, X; Overshiner, C; Wafford, KA; Seidel, W; Wang, XS; Heinz, BA; Swanson, S; Catlow, JT; Bedwell, DW; Monn, JA; Mitch, CH; Ornstein, PL Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity. J Med Chem59:10974-10993 (2016) [PubMed] |
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| More Info.: | Get all data from this article, Assay Method |
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| Metabotropic glutamate receptor 8 |
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| Name: | Metabotropic glutamate receptor 8 |
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| Synonyms: | GPRC1H | GRM8 | GRM8_HUMAN | MGLUR8 | Metabotropic glutamate receptor 8 | metabotropic glutamate 8 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 101759.58 |
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| Organism: | Homo sapiens (Human) |
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| Description: | metabotropic glutamate 8 GRM8 HUMAN::O00222 |
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| Residue: | 908 |
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| Sequence: | MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGER
GVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFV
QALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTA
PELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISR
EIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQS
GHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFA
EFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMH
KDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITN
KSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCER
CEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTF
VIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMC
FSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPH
IIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEA
KPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYI
IIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTY
ISYSNHSI
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|
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| BDBM50558766 |
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| n/a |
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| Name | BDBM50558766 |
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| Synonyms: | CHEMBL4751065 |
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| Type | Small organic molecule |
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| Emp. Form. | C15H16ClF2NO5S |
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| Mol. Mass. | 395.806 |
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| SMILES | Cl.[H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)([C@H](CSc1ccc(F)c(F)c1)[C@H]2O)C(O)=O |r| |
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| Structure | 
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