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TargetMetabotropic glutamate receptor 1
LigandBDBM50177080
Substrate/Competitorn/a
Meas. Tech.ChEMBL_406111 (CHEMBL912698)
IC50 1±n/a nM
Citation Zheng, GZBhatia, PKolasa, TPatel, MEl Kouhen, OFChang, RUchic, MEMiller, LBaker, SLehto, SGHonore, PWetter, JMMarsh, KCMoreland, RBBrioni, JDStewart, AO Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists. Bioorg Med Chem Lett16:4936-40 (2006) [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:
BDBM50177080
n/a
NameBDBM50177080
Synonyms:3-azepan-1-yl-9-dimethylamino-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one | 9-dimethylamino-3-(N-hexamethyleneiminyl)-3H-5-thia-1,3,6-triazafluoren-4-one | CHEMBL386565
TypeSmall organic molecule
Emp. Form.C17H21N5OS
Mol. Mass.343.447
SMILESCN(C)c1ccnc2sc3c(ncn(N4CCCCCC4)c3=O)c12
Structure
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