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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50224390
Substrate
n/a
Meas. Tech.
ChEMBL_450774 (CHEMBL899859)
IC50
0.700000±n/a nM
Citation
 Wu, WL; Burnett, DA; Domalski, M; Greenlee, WJ; Li, C; Bertorelli, R; Fredduzzi, S; Lozza, G; Veltri, A; Reggiani, A Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain. J Med Chem 50:5550-3 (2007) [PubMed]  Article 
Target
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:
MVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGGGQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEEEDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPSHLTAEETPLFLAEPALPKGLPPPLQQQQQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPLQLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPDDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL
  
Inhibitor
Name:
BDBM50224390
Synonyms:
8-(4-methylphenyl)-1h-pyrrolo[2'',3'':4',5']pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-7(8H)-one | CHEMBL393705
Type:
Small organic molecule
Emp. Form.:
C18H12N4OS
Mol. Mass.:
332.379
SMILES:
Cc1ccc(cc1)-n1cnc2c(sc3ncc4cc[nH]c4c23)c1=O
Structure:
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