Target
Metabotropic glutamate receptor 5
Ligand
BDBM50172123
Substrate
n/a
Meas. Tech.
ChEMBL_322406 (CHEMBL871882)
IC50
0.9±n/a nM
Citation
 Chua, PCNagasawa, JYBleicher, LSMunoz, BSchweiger, EJTehrani, LAnderson, JJCramer, MChung, JGreen, MDKing, CDReyes-Manalo, GCosford, ND Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett 15:4589-93 (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:
BDBM50172123
Synonyms:
3-Chloro-5-(3-pyridin-2-ylethynyl-cyclohex-2-enyloxy)-pyridine | CHEMBL381192
Type:
Small organic molecule
Emp. Form.:
C18H15ClN2O
Mol. Mass.:
310.778
SMILES:
Clc1cncc(OC2CCCC(=C2)C#Cc2ccccn2)c1 |c:11|
Structure:
Search PDB for entries with ligand similarity: