Target
Metabotropic glutamate receptor 5
Ligand
BDBM50084137
Substrate
n/a
Ki
28±n/a nM
Comments
PDSP_3235
Citation
 Porter, RHJaeschke, GSpooren, WBallard, TMBüttelmann, BKolczewski, SPeters, JUPrinssen, EWichmann, JVieira, EMühlemann, AGatti, SMutel, VMalherbe, P Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther 315:711-21 (2005) [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:
BDBM50084137
Synonyms:
2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-phenylethynyl-pyridine | 2-Methyl-6-phenylethynyl-pyridine(MPEP) | 2-methyl-6-(2-phenylethynyl)pyridine | 2-methyl-6-(phenyl-ethynyl)pyridine | 2-methyl-6-(phenylethynyl)-pyridine | 6-methyl-2-(2-phenylethynyl)pyridine | CHEMBL1788108 | CHEMBL66654 | MPEP | US10618900, No. MPEP | [3H]-2-methyl-6-(phenylethynyl)-pyridine
Type:
Small organic molecule
Emp. Form.:
C14H11N
Mol. Mass.:
193.2438
SMILES:
Cc1cccc(n1)C#Cc1ccccc1
Structure:
Search PDB for entries with ligand similarity: