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Target
Isoform 1 of Metabotropic glutamate receptor 5 (5a)
Ligand
BDBM198916
Substrate
n/a
Meas. Tech.
Intracellular Ca2+ Mobilization Assay
Temperature
310.15±n/a K
EC50
10±n/a nM
Comments
extracted
Citation
 Jaeschke, G; Lindemann, L; Stadler, H; Vieira, E Arylethynyl derivatives US Patent  US9221802 Publication Date 12/29/2015 
Target
Name:
Isoform 1 of Metabotropic glutamate receptor 5 (5a)
Synonyms:
GPRC1E | GRM5 | GRM5_HUMAN | MGLUR5 | Metabotropic glutamate receptor 5 | Metabotropic glutamate receptor 5 (5a) | Metabotropic glutamate receptor 5 (mGlu5a) | Metabotropic glutamate receptor 5 (mGluR5a) | Metabotropic glutamate receptor 5a (mGluR5) | Metabotropic glutamate receptor 5a (mGluR5a) | Metabotropic glutamate receptor subtype 5 (mGluR5)
Type:
Enzyme
Mol. Mass.:
128885.13
Organism:
Homo sapiens (Human)
Description:
P41594-2
Residue:
1180
Sequence:
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQHRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVVFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRGLGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPSPISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAARESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
  
Inhibitor
Name:
BDBM198916
Synonyms:
US9221802, Ex. 2
Type:
Small organic molecule
Emp. Form.:
C20H17FN2O2
Mol. Mass.:
336.3596
SMILES:
Fc1cccc(c1)C#Cc1ccc(nc1)N1[C@@H]2CCC[C@@H]2COC1=O |r|
Structure:
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