Reaction Details |
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Target | Metabotropic glutamate receptor 5 |
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Ligand | BDBM50177081 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_430990 (CHEMBL916418) |
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Ki | 2300±n/a nM |
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Citation | Zheng, GZ; Bhatia, P; Daanen, J; Kolasa, T; Patel, M; Latshaw, S; El Kouhen, OF; Chang, R; Uchic, ME; Miller, L; Nakane, M; Lehto, SG; Honore, MP; Moreland, RB; Brioni, JD; Stewart, AO Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J Med Chem48:7374-88 (2005) [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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BDBM50177081 |
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n/a |
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Name | BDBM50177081 |
Synonyms: | 3-(2,4-Dichloro-phenyl)-9-dimethylamino-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one | 9-dimethylamino-3-(2,4-dichlorophenyl)-3H-5-thia-1,3,6-triazafluoren-4-one | CHEMBL224898 |
Type | Small organic molecule |
Emp. Form. | C17H12Cl2N4OS |
Mol. Mass. | 391.274 |
SMILES | CN(C)c1ccnc2sc3c(ncn(-c4ccc(Cl)cc4Cl)c3=O)c12 |
Structure |
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