Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 2
Ligand
BDBM277161
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
21200±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:
BDBM277161
Synonyms:
(S) or (R)-4-[1- (difluoromethyl)-1H- pyrazol-4-yl]-7-{(1R)-1-[2- (trifluoromethyl)pyridin-4- yl]ethyl}-5,6,7,8- tetrahydro-1,7- naphthyridine-2- carboxamide | US10072003, Example 7-3A | US10072003, Example 7-3B
Type:
Small organic molecule
Emp. Form.:
C21H19F5N6O
Mol. Mass.:
466.4072
SMILES:
CC(N1CCc2c(C1)nc(cc2-c1cnn(c1)C(F)F)C(N)=O)c1ccnc(c1)C(F)(F)F