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Target
Metabotropic glutamate receptor 8
Ligand
BDBM50134466
Substrate
n/a
Meas. Tech.
ChEMBL_1544997 (CHEMBL3749862)
EC50
>10000±n/a nM
Citation
 Conde-Ceide, S; Alcázar, J; Alonso de Diego, SA; López, S; Martín-Martín, ML; Martínez-Viturro, CM; Pena, MA; Tong, HM; Lavreysen, H; Mackie, C; Bridges, TM; Daniels, JS; Niswender, CM; Jones, CK; Macdonald, GJ; Steckler, T; Conn, PJ; Stauffer, SR; Lindsley, CW; Bartolomé-Nebreda, JM Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. Bioorg Med Chem Lett 26:429-34 (2016) [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:
BDBM50134466
Synonyms:
CHEMBL3747116
Type:
Small organic molecule
Emp. Form.:
C19H16FN3O2
Mol. Mass.:
337.3476
SMILES:
Fc1ccc(cc1)N1CCn2nc(OCc3ccccc3)cc2C1=O
Structure:
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