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Target
Metabotropic glutamate receptor 2
Ligand
BDBM50332968
Substrate
n/a
Meas. Tech.
ChEMBL_696926 (CHEMBL1639554)
IC50
15±n/a nM
Citation
 Woltering, TJ; Wichmann, J; Goetschi, E; Knoflach, F; Ballard, TM; Huwyler, J; Gatti, S Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists. Bioorg Med Chem Lett 20:6969-74 (2010) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 2
Synonyms:
GPRC1B | GRM2 | GRM2_HUMAN | MGLUR2 | Metabotropic glutamate receptor | glutamate receptor, metabotropic 2 precursor | mGlu2 | metabotropic glutamate 2
Type:
Enzyme
Mol. Mass.:
95584.88
Organism:
Homo sapiens (Human)
Description:
Q14416
Residue:
872
Sequence:
MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQRLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGALESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYKDFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAARASSSLGQGSGSQFVPTVCNGREVVDSTTSSL
  
Inhibitor
Name:
BDBM50332968
Synonyms:
7-ethoxy-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one | CHEMBL1629866
Type:
Small organic molecule
Emp. Form.:
C24H20F3N3O2
Mol. Mass.:
439.4297
SMILES:
CCOc1cc2N=C(CC(=O)Nc2cc1C(F)(F)F)c1cccc(c1)-c1ccnc(C)c1 |c:6|
Structure:
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