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Target
Isoform 1 of Metabotropic glutamate receptor 5 (5a)
Ligand
BDBM222736
Substrate
n/a
Meas. Tech.
Intracellular Ca2+ Mobilization Assay
Temperature
310.15±n/a K
EC50
35±n/a nM
Comments
extracted
Citation
 Green, L; Guba, W; Jaeschke, G; Jolidon, S; Lindemann, L; Ricci, A; Rueher, D; Stadler, H; Vieira, E Arlethynyl derivatives US Patent  US9315498 Publication Date 4/19/2016 
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:
BDBM222736
Synonyms:
US9315498, 24
Type:
Small organic molecule
Emp. Form.:
C18H14FN3O2
Mol. Mass.:
323.3211
SMILES:
Fc1cncc(c1)C#Cc1ccc(nc1)N1[C@@H]2CCC[C@@H]2OC1=O |r|
Structure:
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