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TargetMetabotropic glutamate receptor 1
LigandBDBM50224401
Substrate/Competitorn/a
Meas. Tech.ChEMBL_450777 (CHEMBL899862)
Ki 20±n/a nM
Citation Wu, WLBurnett, DADomalski, MGreenlee, WJLi, CBertorelli, RFredduzzi, SLozza, GVeltri, AReggiani, A Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain. J Med Chem50:5550-3 (2007) [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:
BDBM50224401
n/a
NameBDBM50224401
Synonyms:8-(4-chlorophenyl)-1h-pyrazolo[3'',4'':4',5']pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-7(8H)-one | CHEMBL238263
TypeSmall organic molecule
Emp. Form.C16H8ClN5OS
Mol. Mass.353.786
SMILESClc1ccc(cc1)-n1cnc2c(sc3ncc4c[nH]nc4c23)c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: