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TargetMetabotropic glutamate receptor 1
LigandBDBM50401676
Substrate/Competitorn/a
Meas. Tech.ChEMBL_884984 (CHEMBL2211244)
Ki 14.5±n/a nM
Citation Brumfield, SKorakas, PSilverman, LSTulshian, DMatasi, JJQiang, LBennett, CEBurnett, DAGreenlee, WJKnutson, CEWu, WLSasikumar, TKDomalski, MBertorelli, RGrilli, MLozza, GReggiani, ALi, C Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain. Bioorg Med Chem Lett22:7223-6 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Metabotropic glutamate receptor 1
Name:Metabotropic glutamate receptor 1
Synonyms:GRM1_RAT | Gprc1a | Grm1 | Metabotropic Glutamate 1a | Metabotropic glutamate receptor | Metabotropic glutamate receptor 1 | Mglur1 | metabotropic glutamate 1 | metabotropic glutamate 1/5-D | metabotropic glutamate 1/DA | metabotropic glutamate receptor 1 isoform alpha precursor
Type:Enzyme Catalytic Domain
Mol. Mass.:133240.47
Organism:RAT
Description:metabotropic glutamate 1/2 0 RAT::P23385
Residue:1199
Sequence:
MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAE
KVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSI
EFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDI
PQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESG
MDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLL
SAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLD
TNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAM
AHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYD
IMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGE
VSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFS
CLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQ
RLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTL
VVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPAN
FNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIA
KPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGG
RQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEE
DNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQ
QPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQ
HLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTAS
KLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50401676
n/a
NameBDBM50401676
Synonyms:CHEMBL2205915
TypeSmall organic molecule
Emp. Form.C18H15N5O2S
Mol. Mass.365.409
SMILESCOc1ccc(cc1)-n1cnc2c(sc3ncnc(NC4CC4)c23)c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: