Target
Metabotropic glutamate receptor 1
Ligand
BDBM50163617
Substrate
n/a
Meas. Tech.
ChEMBL_305830 (CHEMBL829572)
IC50
2±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:
BDBM50163617
Synonyms:
(2,3-Dihydro-thieno[2,3-b]quinolin-6-yl)-(4-methoxy-cyclohexyl)-methanone | CHEMBL175463
Type:
Small organic molecule
Emp. Form.:
C19H21NO2S
Mol. Mass.:
327.441
SMILES:
CO[C@H]1CC[C@H](CC1)C(=O)c1ccc2nc3SCCc3cc2c1 |wU:5.8,2.1,(-8.35,-.82,;-7.02,-1.59,;-5.67,-.82,;-5.67,.72,;-4.36,1.49,;-3.03,.72,;-3.03,-.82,;-4.36,-1.59,;-1.68,1.49,;-1.7,3.03,;-.34,.74,;-.34,-.82,;.98,-1.57,;2.31,-.78,;3.66,-1.56,;4.98,-.75,;6.32,-1.5,;7.65,-.71,;7.65,.83,;4.97,.79,;3.62,1.54,;2.31,.75,;.96,1.51,)|
Structure:
Search PDB for entries with ligand similarity: