| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 5 |
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| Ligand | BDBM50448155 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1292286 (CHEMBL3124717) |
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| Ki | 8.1±n/a nM |
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| Citation |  Zhang, L; Balan, G; Barreiro, G; Boscoe, BP; Chenard, LK; Cianfrogna, J; Claffey, MM; Chen, L; Coffman, KJ; Drozda, SE; Dunetz, JR; Fonseca, KR; Galatsis, P; Grimwood, S; Lazzaro, JT; Mancuso, JY; Miller, EL; Reese, MR; Rogers, BN; Sakurada, I; Skaddan, M; Smith, DL; Stepan, AF; Trapa, P; Tuttle, JB; Verhoest, PR; Walker, DP; Wright, AS; Zaleska, MM; Zasadny, K; Shaffer, CL Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator. J Med Chem57:861-77 (2014) [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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| BDBM50448155 |
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| n/a |
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| Name | BDBM50448155 |
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| Synonyms: | CHEMBL3122217 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H17N7O |
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| Mol. Mass. | 335.3632 |
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| SMILES | Cc1c(cnn1C)-c1nn(C)c2nc(OCc3ccccn3)cnc12 |
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| Structure | 
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