Reaction Details |
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Target | Metabotropic glutamate receptor 5 |
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Ligand | BDBM50071334 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1469541 (CHEMBL3412489) |
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Ki | 90±n/a nM |
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Citation | Jaeschke, G; Kolczewski, S; Spooren, W; Vieira, E; Bitter-Stoll, N; Boissin, P; Borroni, E; Büttelmann, B; Ceccarelli, S; Clemann, N; David, B; Funk, C; Guba, W; Harrison, A; Hartung, T; Honer, M; Huwyler, J; Kuratli, M; Niederhauser, U; Pähler, A; Peters, JU; Petersen, A; Prinssen, E; Ricci, A; Rueher, D; Rueher, M; Schneider, M; Spurr, P; Stoll, T; Tännler, D; Wichmann, J; Porter, RH; Wettstein, JG; Lindemann, L Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. J Med Chem58:1358-71 (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: | GPRC1E | GRM5 | GRM5_HUMAN | MGLUR5 | metabotropic glutamate 5 | metabotropic glutamate 5a |
Type: | Enzyme |
Mol. Mass.: | 132484.72 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 1212 |
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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BDBM50071334 |
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n/a |
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Name | BDBM50071334 |
Synonyms: | CHEMBL3410216 |
Type | Small organic molecule |
Emp. Form. | C19H14N4 |
Mol. Mass. | 298.3413 |
SMILES | Cc1nc(cn1-c1cccc(c1)C#N)C#Cc1ccnc(C)c1 |
Structure |
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