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TargetMetabotropic glutamate receptor 5
LigandBDBM50395923
Substrate/Competitorn/a
Meas. Tech.ChEMBL_858345 (CHEMBL2168560)
IC50 26±n/a nM
Citation Raboisson, PBreitholtz-Emanuelsson, ADahllöf, HEdwards, LHeaton, WLIsaac, MJarvie, KKers, AMinidis, ABNordmark, ASheehan, SMSlassi, AStröm, PTerelius, YWensbo, DWilson, JMXin, TMcLeod, DA Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett22:6974-9 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Metabotropic glutamate receptor 5
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50395923
n/a
NameBDBM50395923
Synonyms:CHEMBL2164550
TypeSmall organic molecule
Emp. Form.C14H6F2N4O
Mol. Mass.284.2204
SMILESFc1ccc(nc1)-c1noc(n1)-c1cc(F)cc(c1)C#N
Structure
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