Reaction Details |
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Target | Metabotropic glutamate receptor 5 |
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Ligand | BDBM50257080 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1688692 |
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IC50 | 7.2±n/a nM |
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Citation | Felts, AS; Rodriguez, AL; Blobaum, AL; Morrison, RD; Bates, BS; Thompson Gray, A; Rook, JM; Tantawy, MN; Byers, FW; Chang, S; Venable, DF; Luscombe, VB; Tamagnan, GD; Niswender, CM; Daniels, JS; Jones, CK; Conn, PJ; Lindsley, CW; Emmitte, KA Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem60:5072-5085 (2017) [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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BDBM50257080 |
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n/a |
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Name | BDBM50257080 |
Synonyms: | CHEMBL4096818 |
Type | Small organic molecule |
Emp. Form. | C17H12ClFN4O2 |
Mol. Mass. | 358.754 |
SMILES | Cc1cc(Oc2cncc(Cl)c2)cc(n1)C(=O)Nc1ccc(F)cn1 |
Structure |
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