Target
Metabotropic glutamate receptor 1
Ligand
BDBM50163610
Substrate
n/a
Meas. Tech.
ChEMBL_305883 (CHEMBL874546)
IC50
450±n/a nM
Citation
 Mabire, DCoupa, SAdelinet, CPoncelet, ASimonnet, YVenet, MWouters, RLesage, ASVan Beijsterveldt, LBischoff, F Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J Med Chem 48:2134-53 (2005) [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:
BDBM50163610
Synonyms:
(4-Ethyl-1,2,3,9b-tetraaza-cyclopenta[a]naphthalen-7-yl)-(4-methoxy-cyclohexyl)-methanone | CHEMBL176068
Type:
Small organic molecule
Emp. Form.:
C19H22N4O2
Mol. Mass.:
338.4036
SMILES:
CCc1cc2cc(ccc2n2nnnc12)C(=O)[C@@H]1CC[C@@H](CC1)OC |wU:17.19,20.26,(7.33,1,;5.98,1.74,;4.65,.97,;3.3,1.72,;1.98,.93,;.64,1.68,;-.67,.9,;-.67,-.64,;.66,-1.41,;1.99,-.61,;3.34,-1.38,;3.69,-2.88,;5.23,-3.02,;5.83,-1.59,;4.67,-.59,;-2.01,1.65,;-2.02,3.19,;-3.34,.88,;-4.68,1.65,;-5.99,.88,;-5.99,-.66,;-4.68,-1.43,;-3.34,-.66,;-7.33,-1.43,;-8.67,-.66,)|
Structure:
Search PDB for entries with ligand similarity: