| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 5 |
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| Ligand | BDBM174258 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1627459 (CHEMBL3869980) |
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| Ki | 15±n/a nM |
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| Citation |  Degnan, AP; Maxwell, D; Balakrishnan, A; Brown, JM; Easton, A; Gulianello, M; Hanumegowda, U; Hill-Drzewi, M; Miller, R; Santone, KS; Senapati, A; Shields, EE; Sivarao, DV; Westphal, R; Whiterock, VJ; Zhuo, X; Bronson, JJ; Macor, JE Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential. Bioorg Med Chem Lett26:5871-5876 (2016) [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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| BDBM174258 |
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| n/a |
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| Name | BDBM174258 |
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| Synonyms: | US9688669, Example 89 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H17FN2O2 |
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| Mol. Mass. | 336.3596 |
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| SMILES | Fc1cccc(c1)[C@H]1OC(=O)N[C@@H]1c1cncc(c1)C#CC1CCC1 |r| |
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| Structure | 
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