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Target
Metabotropic glutamate receptor 2
Ligand
BDBM277189
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
6500±n/a nM
Citation
 Arasappan, A; Bungard, CJ; Frie, JL; Han, Y; Hoyt, SB; Manley, PJ; Meissner, RS; Perkins, JJ; Sebhat, IK; Wilkening, RR; Leavitt, KJ Tetrahydronaphthyridine derivatives as mGluR2-negative allosteric modulators, compositions, and their use US Patent  US10072003 Publication Date 9/11/2018 
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:
BDBM277189
Synonyms:
4-(4-chloro-2,6-difluorophenyl)-7-{[2- (trifluoromethyl)pyrimidin-4-yl]methyl}- 5,6,7,8-tetrahydro-1,7-naphthyridine-2- carboxamide | US10072003, Example 11-9
Type:
Small organic molecule
Emp. Form.:
C21H15ClF5N5O
Mol. Mass.:
483.822
SMILES:
NC(=O)c1cc(c2CCN(Cc3ccnc(n3)C(F)(F)F)Cc2n1)-c1c(F)cc(Cl)cc1F |(-8,-3.08,;-6.67,-3.85,;-6.67,-5.39,;-5.33,-3.08,;-5.33,-1.54,;-4,-.77,;-2.67,-1.54,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;2.67,-3.08,;2.67,-1.54,;4,-.77,;5.33,-1.54,;5.33,-3.08,;4,-3.85,;6.67,-3.85,;8,-3.08,;6.67,-5.39,;8,-4.62,;-1.33,-3.85,;-2.67,-3.08,;-4,-3.85,;-4,.77,;-5.33,1.54,;-6.67,.77,;-5.33,3.08,;-4,3.85,;-4,5.39,;-2.67,3.08,;-2.67,1.54,;-1.33,.77,)|
Structure:
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