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Target
Guanine nucleotide-binding protein subunit alpha-15 [Y147C]/Metabotropic glutamate receptor 2
Ligand
BDBM213144
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
5±n/a nM
Citation
 Bungard, CJ; Converso, A; Hanney, B; Hartingh, TJ; Manley, PJ; Meissner, RS; Perkins, JJ; Rudd, MT Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use US Patent  US9278960 Publication Date 3/8/2016 
Target
Name:
Guanine nucleotide-binding protein subunit alpha-15 [Y147C]/Metabotropic glutamate receptor 2
Synonyms:
Guanine nucleotide-binding protein subunit alpha-15/Metabotropic glutamate receptor 2 | mGluR2 and G alpha 16
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Guanine nucleotide-binding protein subunit alpha-15
Synonyms:
G protein alpha 16 | G-protein subunit alpha-16 | G-protein subunit alpha-16 (G alpha-16) | GNA15 | GNA15_HUMAN | GNA16 | Guanine nucleotide-binding protein subunit alpha-15 [Y147C]
Type:
Protein
Mol. Mass.:
43577.62
Organism:
Homo sapiens (Human)
Description:
P30679
Residue:
374
Sequence:
MARSLTWRCCPWCLTEDEKAAARVDQEINRILLEQKKQDRGELKLLLLGPGESGKSTFIKQMRIIHGAGYSEEERKGFRPLVYQNIFVSMRAMIEAMERLQIPFSRPESKHHASLVMSQDPYKVTTFEKRYAAAMQWLWRDAGIRACYERRREFHLLDSAVYYLSHLERITEEGYVPTAQDVLRSRMPTTGINEYCFSVQKTNLRIVDVGGQKSERKKWIHCFENVIALIYLASLSEYDQCLEENNQENRMKESLALFGTILELPWFKSTSVILFLNKTDILEEKIPTSHLATYFPSFQGPKQDAEAAKRFILDMYTRMYTGCVDGPEGSKKGARSRRLFSHYTCATDTQNIRKVFKDVRDSVLARYLDEINLL
  
Inhibitor
Name:
BDBM213144
Synonyms:
US9278960, 8-51 | US9636337, 8-51
Type:
Small organic molecule
Emp. Form.:
C24H20F2N4O2
Mol. Mass.:
434.438
SMILES:
COc1cc(F)c(c(F)c1)-c1cc(nc2cc(CCc3cnc(C)nc3)ccc12)C(N)=O |(5.33,-6.16,;4,-5.39,;4,-3.85,;5.33,-3.08,;5.33,-1.54,;6.67,-.77,;4,-.77,;2.67,-1.54,;1.33,-.77,;2.67,-3.08,;4,.77,;5.33,1.54,;5.33,3.08,;4,3.85,;2.67,3.08,;1.33,3.85,;,3.08,;-1.33,3.85,;-2.67,3.08,;-4,3.85,;-4,5.39,;-5.33,6.16,;-6.67,5.39,;-8,6.16,;-6.67,3.85,;-5.33,3.08,;,1.54,;1.33,.77,;2.67,1.54,;6.67,3.85,;8,3.08,;6.67,5.39,)|
Structure:
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