Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 2
Ligand
BDBM277134
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
23000±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:
BDBM277134
Synonyms:
4-(3-cyclopropylisothiazol-5-yl)-7-{[2- (difluoromethoxy)pyridin-4-yl]methyl}- 5,6,7,8-tetrahydro-1,7-naphthyridine-2- carboxamide | US10072003, Example 2-27
Type:
Small organic molecule
Emp. Form.:
C22H21F2N5O2S
Mol. Mass.:
457.496
SMILES:
NC(=O)c1cc(-c2cc(ns2)C2CC2)c2CCN(Cc3ccnc(OC(F)F)c3)Cc2n1