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Target
Metabotropic glutamate receptor 5
Ligand
BDBM50156082
Substrate
n/a
Meas. Tech.
ChEMBL_454009 (CHEMBL903196)
EC50
<1000±n/a nM
Citation
 Zhao, Z; Wisnoski, DD; O'Brien, JA; Lemaire, W; Williams, DL; Jacobson, MA; Wittman, M; Ha, SN; Schaffhauser, H; Sur, C; Pettibone, DJ; Duggan, ME; Conn, PJ; Hartman, GD; Lindsley, CW Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg Med Chem Lett 17:1386-91 (2007) [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:
BDBM50156082
Synonyms:
CHEMBL362969 | N-(4-bromo-2-((1,3-dioxoisoindolin-2-yl)methyl)phenyl)picolinamide | Pyridine-2-carboxylic acid [4-bromo-2-(1,3-dioxo-1,3-dihydro-isoindol-2-ylmethyl)-phenyl]-amide
Type:
Small organic molecule
Emp. Form.:
C21H14BrN3O3
Mol. Mass.:
436.258
SMILES:
Brc1ccc(NC(=O)c2ccccn2)c(CN2C(=O)c3ccccc3C2=O)c1
Structure:
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