Reaction Details |
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Target | Metabotropic glutamate receptor 5 |
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Ligand | BDBM50064474 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1464920 (CHEMBL3404390) |
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IC50 | 132±n/a nM |
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Citation | Martín-Martín, ML; Bartolomé-Nebreda, JM; Conde-Ceide, S; Alonso de Diego, SA; López, S; Martínez-Viturro, CM; Tong, HM; Lavreysen, H; Macdonald, GJ; Steckler, T; Mackie, C; Bridges, TM; Daniels, JS; Niswender, CM; Noetzel, MJ; Jones, CK; Conn, PJ; Lindsley, CW; Stauffer, SR Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett25:1310-7 (2015) [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 |
Synonyms: | GRM5_RAT | Gprc1e | Grm5 | Metabotropic glutamate receptor | Mglur5 | metabotropic glutamate 5 | metabotropic glutamate 5/1-C | metabotropic glutamate 5/1-F | metabotropic glutamate 5a |
Type: | Enzyme |
Mol. Mass.: | 131900.14 |
Organism: | Rattus norvegicus (Rat) |
Description: | P31424 |
Residue: | 1203 |
Sequence: | MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS
EEEEGLVRCVDGSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSD
KTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGIC
IAHSYKIYSNAGEQSFDKLLKKLRSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLL
LGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNLRNPWFQEFWQH
RFQCRLEGFAQENSKYNKTCNSSLTLRTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPG
YAGLCDAMKPIDGRKLLDSLMKTNFTGVSGDMILFDENGDSPGRYEIMNFKEMGKDYFDY
INVGSWDNGELKMDDDEVWSKKNNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENE
YVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVIF
IIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSA
LVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMH
DYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTT
CIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTST
VVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGN
GGRATMSSSNGKSVTWAQNEKSTRGQHLWQRLSVHINKKENPNQTAVIKPFPKSTENRGP
GAAAGGGSGPGVAGAGNAGCTATGGPEPPDAGPKALYDVAEAEESFPAAARPRSPSPIST
LSHLAGSAGRTDDDAPSLHSETAARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAA
TPGPPGTPICSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQGATGVSPAQETPTGAE
SAPGKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSS
SSL
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BDBM50064474 |
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n/a |
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Name | BDBM50064474 |
Synonyms: | CHEMBL3401204 |
Type | Small organic molecule |
Emp. Form. | C19H15ClFN3O2 |
Mol. Mass. | 371.793 |
SMILES | Fc1ccc(cc1)N1CCc2nc(COc3ccccc3)c(Cl)n2C1=O |
Structure |
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