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Target
Metabotropic glutamate receptor 8
Ligand
BDBM50601004
Substrate
n/a
Meas. Tech.
ChEMBL_2235664 (CHEMBL5149436)
EC50
>1000±n/a nM
Citation
 Yuan, G; Dhaynaut, M; Guehl, NJ; Afshar, S; Huynh, D; Moon, SH; Iyengar, SM; Jain, MK; Pickett, JE; Kang, HJ; Ondrechen, MJ; El Fakhri, G; Normandin, MD; Brownell, AL Design, Synthesis, and Characterization of [ J Med Chem 65:9939-9954 (2022) [PubMed] 
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:
BDBM50601004
Synonyms:
CHEMBL5202739
Type:
Small organic molecule
Emp. Form.:
C22H20F5N5O
Mol. Mass.:
465.4191
SMILES:
Fc1ccc(N2CCN(CC2)C(=O)c2cnc3n(CC4CC4)ncc3c2C(F)(F)F)c(F)c1
Structure:
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