| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 5 |
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| Ligand | BDBM50214084 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_456242 (CHEMBL888252) |
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| IC50 | >100000±n/a nM |
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| Citation |  Wang, X; Kolasa, T; El Kouhen, OF; Chovan, LE; Black-Shaefer, CL; Wagenaar, FL; Garton, JA; Moreland, RB; Honore, P; Lau, YY; Dandliker, PJ; Brioni, JD; Stewart, AO Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett17:4303-7 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Metabotropic glutamate receptor 5 |
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| Name: | Metabotropic glutamate receptor 5 |
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| Synonyms: | GPRC1E | GRM5 | GRM5_HUMAN | MGLUR5 | metabotropic glutamate 5 | metabotropic glutamate 5a |
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| Type: | Enzyme |
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| Mol. Mass.: | 132484.72 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 1212 |
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| Sequence: | MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS
EEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLS
DKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGI
CIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFL
LLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQ
HRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP
GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFD
YINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKEN
EYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVV
FIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYS
ALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIM
HDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYT
TCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS
TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMG
NGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRG
LGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPS
PISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMML
STAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAA
RESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTL
IIRDYTQSSSSL
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| BDBM50214084 |
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| n/a |
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| Name | BDBM50214084 |
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| Synonyms: | 6-methyl-1-phenyl-5-(4-(trifluoromethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one | CHEMBL248210 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H13F3N4O2 |
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| Mol. Mass. | 386.3273 |
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| SMILES | Cc1nc2n(ncc2c(=O)n1-c1ccc(OC(F)(F)F)cc1)-c1ccccc1 |
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| Structure | 
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