Reaction Details |
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Target | Metabotropic glutamate receptor 1 |
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Ligand | BDBM50143085 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1550577 (CHEMBL3762431) |
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EC50 | >10000±n/a nM |
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Citation | Garcia-Barrantes, PM; Cho, HP; Metts, AM; Blobaum, AL; Niswender, CM; Conn, PJ; Lindsley, CW Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorg Med Chem Lett26:751-6 (2016) [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: | GPRC1A | GRM1 | GRM1_HUMAN | MGLUR1 | Metabotropic Glutamate 1a | metabotropic glutamate 1 |
Type: | Enzyme |
Mol. Mass.: | 132358.19 |
Organism: | Homo sapiens (Human) |
Description: | Q13255 |
Residue: | 1194 |
Sequence: | MVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAE
KVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSI
EFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDI
PQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESG
MDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLL
SAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLD
TNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAM
AHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYD
IMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGE
VSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFS
CLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQ
RLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTL
VVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPAN
FNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIA
KPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGG
GQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEE
EDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPSHLTAEETPLFLAEPALPKGLPPPLQQQ
QQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPL
QLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPD
DSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL
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BDBM50143085 |
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n/a |
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Name | BDBM50143085 |
Synonyms: | CHEMBL3759846 |
Type | Small organic molecule |
Emp. Form. | C18H12ClN5O3 |
Mol. Mass. | 381.773 |
SMILES | Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 |
Structure |
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