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Target
Metabotropic glutamate receptor 8
Ligand
BDBM50255389
Substrate
n/a
Meas. Tech.
ChEMBL_1687020 (CHEMBL4037499)
EC50
1250±n/a nM
Citation
 Selvam, C; Lemasson, IA; Brabet, I; Oueslati, N; Karaman, B; Cabaye, A; Tora, AS; Commare, B; Courtiol, T; Cesarini, S; McCort-Tranchepain, I; Rigault, D; Mony, L; Bessiron, T; McLean, H; Leroux, FR; Colobert, F; Daniel, H; Goupil-Lamy, A; Bertrand, HO; Goudet, C; Pin, JP; Acher, FC Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem 61:1969-1989 (2018) [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:
BDBM50255389
Synonyms:
CHEMBL4072781
Type:
Small organic molecule
Emp. Form.:
C11H15N2O7P
Mol. Mass.:
318.2198
SMILES:
N[C@@H](CCP(O)(=O)[C@H](O)c1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Structure:
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