Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 8
Ligand
BDBM50064463
Substrate
n/a
Meas. Tech.
ChEMBL_1464935 (CHEMBL3404405)
EC50
>10000±n/a nM
Citation
 Martín-Martín, ML; Bartolomé-Nebreda, JM; Conde-Ceide, S; Alonso de Diego, SA; López, S; Martínez-Viturro, CM; Tong, HM; Lavreysen, H; Macdonald, GJ; Steckler, T; Mackie, C; Bridges, TM; Daniels, JS; Niswender, CM; Noetzel, MJ; Jones, CK; Conn, PJ; Lindsley, CW; Stauffer, SR Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett 25:1310-7 (2015) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 8
Synonyms:
GPRC1H | GRM8 | GRM8_HUMAN | MGLUR8 | Metabotropic glutamate receptor 8 | metabotropic glutamate 8
Type:
Enzyme Catalytic Domain
Mol. Mass.:
101759.58
Organism:
Homo sapiens (Human)
Description:
metabotropic glutamate 8 GRM8 HUMAN::O00222
Residue:
908
Sequence:
MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITNKSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHIIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
  
Inhibitor
Name:
BDBM50064463
Synonyms:
CHEMBL3401177
Type:
Small organic molecule
Emp. Form.:
C19H14FN3O2
Mol. Mass.:
335.3318
SMILES:
Fc1ccc(cc1)-n1ccc2nc(COc3ccccc3)cn2c1=O
Structure:
Search PDB for entries with ligand similarity: