| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 2 |
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| Ligand | BDBM50399088 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1616782 (CHEMBL3858851) |
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| EC50 | 4.8±n/a nM |
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| Citation |  Cid, JM; Tresadern, G; Vega, JA; de Lucas, AI; Del Cerro, A; Matesanz, E; Linares, ML; García, A; Iturrino, L; Pérez-Benito, L; Macdonald, GJ; Oehlrich, D; Lavreysen, H; Peeters, L; Ceusters, M; Ahnaou, A; Drinkenburg, W; Mackie, C; Somers, M; Trabanco, AA Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). J Med Chem59:8495-507 (2016) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Metabotropic glutamate receptor 2 |
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| Name: | Metabotropic glutamate receptor 2 |
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| Synonyms: | GPRC1B | GRM2 | GRM2_HUMAN | MGLUR2 | Metabotropic glutamate receptor | glutamate receptor, metabotropic 2 precursor | mGlu2 | metabotropic glutamate 2 |
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| Type: | Enzyme |
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| Mol. Mass.: | 95584.88 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q14416 |
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| Residue: | 872 |
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| Sequence: | MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQ
RLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHI
CPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDY
FARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEK
VGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGAL
ESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQR
DCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYK
DFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTL
DTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADC
GLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKA
SGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARI
FGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLR
CNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIF
YVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAA
RASSSLGQGSGSQFVPTVCNGREVVDSTTSSL
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| BDBM50399088 |
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| n/a |
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| Name | BDBM50399088 |
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| Synonyms: | CHEMBL2179319 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H23F3N4 |
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| Mol. Mass. | 400.44 |
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| SMILES | FC(F)(F)c1c(ccn2c(CC3CC3)nnc12)N1CCC(CC1)c1ccccc1 |
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| Structure | 
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