Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 5
Ligand
BDBM50122758
Substrate
n/a
Ki
5.4±n/a nM
Comments
PDSP_4885
Citation
 Porter, RH; Jaeschke, G; Spooren, W; Ballard, TM; Büttelmann, B; Kolczewski, S; Peters, JU; Prinssen, E; Wichmann, J; Vieira, E; Mühlemann, A; Gatti, S; Mutel, V; Malherbe, 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:
GRM5_RAT | Gprc1e | Grm5 | Metabotropic glutamate receptor | Mglur5 | metabotropic glutamate 5 | metabotropic glutamate 5/1-C | metabotropic glutamate 5/1-F | metabotropic glutamate 5a
Type:
Enzyme
Mol. Mass.:
131900.14
Organism:
Rattus norvegicus (Rat)
Description:
P31424
Residue:
1203
Sequence:
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLRSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNLRNPWFQEFWQHRFQCRLEGFAQENSKYNKTCNSSLTLRTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLDSLMKTNFTGVSGDMILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKNNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVIFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSSNGKSVTWAQNEKSTRGQHLWQRLSVHINKKENPNQTAVIKPFPKSTENRGPGAAAGGGSGPGVAGAGNAGCTATGGPEPPDAGPKALYDVAEAEESFPAAARPRSPSPISTLSHLAGSAGRTDDDAPSLHSETAARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAATPGPPGTPICSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQGATGVSPAQETPTGAESAPGKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
  
Inhibitor
Name:
BDBM50122758
Synonyms:
2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2-methylthiazol-4-yl)ethynyl)pyridine | 3-(2-Methyl-thiazol-4-ylethynyl)-pyridine | 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine | 3-[(2-methyl-4-thiazolyl)ethynyl]pyridine | CHEMBL292065 | MTEP
Type:
Small organic molecule
Emp. Form.:
C11H8N2S
Mol. Mass.:
200.26
SMILES:
Cc1nc(cs1)C#Cc1cccnc1
Structure:
Search PDB for entries with ligand similarity: