Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 8
Ligand
BDBM50283478
Substrate
n/a
Meas. Tech.
ChEMBL_1725550 (CHEMBL4140828)
EC50
490±n/a nM
Citation
 Abe, M; Seto, M; Gogliotti, RG; Loch, MT; Bollinger, KA; Chang, S; Engelberg, EM; Luscombe, VB; Harp, JM; Bubser, M; Engers, DW; Jones, CK; Rodriguez, AL; Blobaum, AL; Conn, PJ; Niswender, CM; Lindsley, CW Discovery of VU6005649, a CNS Penetrant mGlu ACS Med Chem Lett 8:1110-1115 (2017) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 8
Synonyms:
GRM8_RAT | Gprc1h | Grm8 | Metabotropic glutamate receptor | Metabotropic glutamate receptor 8 (mGlu8) | Mglur8 | glutamate receptor, metabotropic 8 precursor | mGlu8 | metabotropic glutamate 8
Type:
Enzyme
Mol. Mass.:
101886.18
Organism:
Rattus norvegicus (Rat)
Description:
P70579
Residue:
908
Sequence:
MVCEGKRLASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKERCPGYIGLCPRMVTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQINNKSTEYKIIGHWTNQLHLKVEDMQWANREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNINRTGCQRIPIIKLEWHSPWAVVPVFIAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRIFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHTIIDYGEQRTLDPENARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
  
Inhibitor
Name:
BDBM50283478
Synonyms:
CHEMBL4164141
Type:
Small organic molecule
Emp. Form.:
C16H12ClF4N3O
Mol. Mass.:
373.733
SMILES:
COc1cc(F)c(cc1Cl)-c1c(C)nn2c(cc(C)nc12)C(F)(F)F |(37.17,-44.14,;38.18,-42.98,;37.7,-41.52,;38.73,-40.37,;38.23,-38.91,;39.26,-37.76,;36.73,-38.6,;35.71,-39.75,;36.19,-41.21,;35.16,-42.36,;36.25,-37.14,;37.15,-35.9,;38.69,-35.89,;36.24,-34.66,;34.78,-35.14,;33.45,-34.37,;32.12,-35.14,;32.12,-36.68,;30.79,-37.46,;33.45,-37.45,;34.79,-36.67,;33.45,-32.83,;34.79,-32.05,;32.12,-32.05,;33.44,-31.28,)|
Structure:
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