Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 2
Ligand
BDBM277147
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
12900±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
More Info.:
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:
BDBM277147
Synonyms:
(S) or (R)-4-(3- methylpiperidin-1-yl)-7- ((2- (trifluoromethyl)pyridin-4- yl)methyl)-5,6,7,8- tetrahydro-1,7- naphthyridine-2- carboxamide | US10072003, Example 5-5A | US10072003, Example 5-5B
Type:
Small organic molecule
Emp. Form.:
C22H26F3N5O
Mol. Mass.:
433.4699
SMILES:
CC1CCCN(C1)c1cc(nc2CN(Cc3ccnc(c3)C(F)(F)F)CCc12)C(N)=O