Target
Metabotropic glutamate receptor 8
Ligand
BDBM50278930
Substrate
n/a
Meas. Tech.
ChEMBL_545998 (CHEMBL1027702)
IC50
>10000±n/a nM
Citation
 Sharma, SKedrowski, JRook, JMSmith, RLJones, CKRodriguez, ALConn, PJLindsley, CW Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. J Med Chem 52:4103-6 (2009) [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:
BDBM50278930
Synonyms:
2-(m-tolylethynyl)pyrimidine | CHEMBL496882
Type:
Small organic molecule
Emp. Form.:
C13H10N2
Mol. Mass.:
194.2319
SMILES:
Cc1cccc(c1)C#Cc1ncccn1
Structure:
Search PDB for entries with ligand similarity: