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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50163619
Substrate
n/a
Meas. Tech.
ChEMBL_305830 (CHEMBL829572)
IC50
>10000±n/a nM
Citation
 Mabire, D; Coupa, S; Adelinet, C; Poncelet, A; Simonnet, Y; Venet, M; Wouters, R; Lesage, AS; Van Beijsterveldt, L; Bischoff, 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:
BDBM50163619
Synonyms:
CHEMBL558629 | [3-Ethyl-2-(3H-1lambda*4*-thiazol-2-yl)-quinolin-6-yl]-(4-methoxy-cyclohexyl)-methanone
Type:
Small organic molecule
Emp. Form.:
C22H25N2O2S
Mol. Mass.:
381.511
SMILES:
CCc1cc2cc(ccc2nc1-c1[nH+]ccs1)C(=O)C1CCC(CC1)OC |(6.55,1.04,;5.22,1.79,;3.87,1.02,;2.55,1.79,;1.21,1.02,;-.12,1.79,;-1.46,1.02,;-1.46,-.52,;-.13,-1.31,;1.21,-.52,;2.55,-1.31,;3.87,-.52,;5.24,-1.31,;5.4,-2.85,;6.92,-3.17,;7.67,-1.82,;6.65,-.68,;-2.79,1.79,;-2.77,3.35,;-4.14,1.02,;-5.47,1.79,;-6.79,1.02,;-6.79,-.52,;-5.47,-1.3,;-4.14,-.52,;-8.13,-1.3,;-9.47,-.52,)|
Structure:
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