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Target
Metabotropic glutamate receptor 5
Ligand
BDBM571418
Substrate
n/a
Meas. Tech.
Calcium Fluorescence Measurements
IC50
2.02±n/a nM
Citation
 Riva, C; Graziani, D; Longhi, M; Callegari, E; Frigerio, F; Angelico, P Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors US Patent  US11440922 Publication Date 9/13/2022 
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:
BDBM571418
Synonyms:
US11440922, Example 48 | ethyl (3E)-2,2-dimethyl-3- [3-(6-methylpyridin-2- yl)prop-2-yn-1- ylidene]pyrrolidine-1- carboxylate
Type:
Small organic molecule
Emp. Form.:
C18H22N2O2
Mol. Mass.:
298.3795
SMILES:
CCOC(=O)N1CC\C(=C/C#Cc2cccc(C)n2)C1(C)C
Structure:
Search PDB for entries with ligand similarity: