| Reaction Details |
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 | Report a problem with these data |
| Target | Metabotropic glutamate receptor 1 |
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| Ligand | BDBM50190237 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_406111 (CHEMBL912698) |
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| IC50 | 52±n/a nM |
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| Citation |  Zheng, GZ; Bhatia, P; Kolasa, T; Patel, M; El Kouhen, OF; Chang, R; Uchic, ME; Miller, L; Baker, S; Lehto, SG; Honore, P; Wetter, JM; Marsh, KC; Moreland, RB; Brioni, JD; Stewart, 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 |
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| More Info.: | Get all data from this article, Assay Method |
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| Metabotropic glutamate receptor 1 |
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| Name: | Metabotropic glutamate receptor 1 |
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| 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 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 133240.47 |
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| Organism: | RAT |
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| Description: | metabotropic glutamate 1/2 0 RAT::P23385 |
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| Residue: | 1199 |
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| Sequence: | MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAE
KVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSI
EFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDI
PQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESG
MDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLL
SAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLD
TNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAM
AHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYD
IMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGE
VSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFS
CLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQ
RLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTL
VVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPAN
FNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIA
KPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGG
RQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEE
DNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQ
QPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQ
HLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTAS
KLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
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| BDBM50190237 |
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| n/a |
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| Name | BDBM50190237 |
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| Synonyms: | 3-(4-Ethyl-phenyl)-9-[methyl-(2-pyridin-2-yl-ethyl)-amino]-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one | CHEMBL213760 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H23N5OS |
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| Mol. Mass. | 441.548 |
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| SMILES | CCc1ccc(cc1)-n1cnc2c(sc3nccc(N(C)CCc4ccccn4)c23)c1=O |
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| Structure | 
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