Target
Metabotropic glutamate receptor 5
Ligand
BDBM50132611
Substrate
n/a
Meas. Tech.
ChEMBL_1527423 (CHEMBL3636798)
EC50
<31623±n/a nM
Citation
 Malosh, CTurlington, MBridges, TMRook, JMNoetzel, MJVinson, PNSteckler, TLavreysen, HMackie, CBartolomé-Nebreda, JMConde-Ceide, SMartínez-Viturro, CMPiedrafita, MSánchez-Casado, MRMacdonald, GJDaniels, JSJones, CKNiswender, CMConn, PJLindsley, CWStauffer, SR Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorg Med Chem Lett 25:5115-20 (2015) [PubMed]  Article
Target
Name:
Metabotropic glutamate receptor 5
Synonyms:
GPRC1E | GRM5 | GRM5_HUMAN | MGLUR5 | metabotropic glutamate 5 | metabotropic glutamate 5a
Type:
Enzyme
Mol. Mass.:
132484.72
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
1212
Sequence:
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQHRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVVFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRGLGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPSPISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAARESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
  
Inhibitor
Name:
BDBM50132611
Synonyms:
CHEMBL3633973
Type:
Small organic molecule
Emp. Form.:
C15H22N4O
Mol. Mass.:
274.3614
SMILES:
CN(Cc1cc2N(CCCn2n1)C(C)=O)C1C2CC1C2 |(4.32,2.44,;4.95,1.38,;4.2,.04,;2.66,.02,;1.76,1.24,;.3,.77,;-1.03,1.56,;-2.38,.77,;-2.38,-.77,;-1.03,-1.56,;.3,-.77,;1.76,-1.24,;-1.02,3.1,;.05,3.71,;-2.09,3.72,;6.5,1.41,;7.59,2.57,;8.26,1.4,;7.59,.28,;8.74,1.4,)|
Structure:
Search PDB for entries with ligand similarity: