Target
Metabotropic glutamate receptor 1
Ligand
BDBM50163628
Substrate
n/a
Meas. Tech.
ChEMBL_305830 (CHEMBL829572)
IC50
2630±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:
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:
MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGGRQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEEDNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQQPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQHLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTASKLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
  
Inhibitor
Name:
BDBM50163628
Synonyms:
3-Ethyl-2-methoxy-6-[1-(4-methoxy-cyclohexyl)-vinyl]-quinoline | CHEMBL175700
Type:
Small organic molecule
Emp. Form.:
C21H27NO2
Mol. Mass.:
325.4446
SMILES:
CCc1cc2cc(ccc2nc1OC)C(=C)[C@@H]1CC[C@@H](CC1)OC |wU:16.17,19.24,(6.17,2.98,;6.17,1.46,;4.82,.69,;3.5,1.46,;2.16,.69,;.84,1.46,;-.5,.69,;-.5,-.85,;.84,-1.61,;2.16,-.85,;3.5,-1.61,;4.82,-.85,;6.17,-1.64,;6.15,-3.17,;-1.84,1.46,;-1.85,2.98,;-3.17,.69,;-4.51,1.46,;-5.84,.69,;-5.84,-.87,;-4.49,-1.64,;-3.17,-.87,;-7.19,-1.64,;-8.54,-.87,)|
Structure:
Search PDB for entries with ligand similarity: