Reaction Details |
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Target | Metabotropic glutamate receptor 1 |
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Ligand | BDBM50448145 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1292284 (CHEMBL3124715) |
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IC50 | >50000±n/a nM |
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Citation | Zhang, L; Balan, G; Barreiro, G; Boscoe, BP; Chenard, LK; Cianfrogna, J; Claffey, MM; Chen, L; Coffman, KJ; Drozda, SE; Dunetz, JR; Fonseca, KR; Galatsis, P; Grimwood, S; Lazzaro, JT; Mancuso, JY; Miller, EL; Reese, MR; Rogers, BN; Sakurada, I; Skaddan, M; Smith, DL; Stepan, AF; Trapa, P; Tuttle, JB; Verhoest, PR; Walker, DP; Wright, AS; Zaleska, MM; Zasadny, K; Shaffer, CL Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator. J Med Chem57:861-77 (2014) [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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BDBM50448145 |
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n/a |
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Name | BDBM50448145 |
Synonyms: | CHEMBL3122206 |
Type | Small organic molecule |
Emp. Form. | C17H20N6O2 |
Mol. Mass. | 340.3797 |
SMILES | CCN(CC)C(=O)c1nn(C)c2nc(OCc3ccccn3)cnc12 |
Structure |
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