Reaction Details |
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Target | Metabotropic glutamate receptor 1 |
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Ligand | BDBM50197274 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_453190 (CHEMBL902340) |
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Ki | 407±n/a nM |
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Citation | Owen, DR; Dodd, PG; Gayton, S; Greener, BS; Harbottle, GW; Mantell, SJ; Maw, GN; Osborne, SA; Rees, H; Ringer, TJ; Rodriguez-Lens, M; Smith, GF Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. Bioorg Med Chem Lett17:486-90 (2007) [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 |
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
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BDBM50197274 |
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n/a |
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Name | BDBM50197274 |
Synonyms: | (8-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyrazin-2-yl)(4-(pyridin-2-yl)-1,4-diazepan-1-yl)methanone | CHEMBL246890 |
Type | Small organic molecule |
Emp. Form. | C22H28N8O |
Mol. Mass. | 420.5107 |
SMILES | CN1CCN(CC1)c1nccn2cc(nc12)C(=O)N1CCCN(CC1)c1ccccn1 |
Structure |
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