| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 5 |
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| Ligand | BDBM50258612 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_523080 (CHEMBL1004110) |
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| IC50 | 0.81±n/a nM |
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| Citation |  Kulkarni, SS; Zou, MF; Cao, J; Deschamps, JR; Rodriguez, AL; Conn, PJ; Newman, AH Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. J Med Chem52:3563-75 (2009) [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: | GRM5_RAT | Gprc1e | Grm5 | Metabotropic glutamate receptor | Mglur5 | metabotropic glutamate 5 | metabotropic glutamate 5/1-C | metabotropic glutamate 5/1-F | metabotropic glutamate 5a |
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| Type: | Enzyme |
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| Mol. Mass.: | 131900.14 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P31424 |
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| Residue: | 1203 |
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| 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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| BDBM50258612 |
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| n/a |
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| Name | BDBM50258612 |
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| Synonyms: | 3-Fluoro-5-cyano-1-(2-methylthiazol-4-ylethynyl)benzene | CHEMBL446543 |
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| Type | Small organic molecule |
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| Emp. Form. | C13H7FN2S |
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| Mol. Mass. | 242.271 |
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| SMILES | Cc1nc(cs1)C#Cc1cc(F)cc(c1)C#N |
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| Structure | 
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