Target
Metabotropic glutamate receptor 6
Ligand
BDBM50558766
Substrate
n/a
Meas. Tech.
ChEMBL_2064711 (CHEMBL4719964)
IC50
4010±n/a nM
Citation
 Chappell, MDLi, RSmith, SCDressman, BATromiczak, EGTripp, AEBlanco, MJVetman, TQuimby, SJMatt, JBritton, TCFivush, AMSchkeryantz, JMMayhugh, DErickson, JABures, MGJaramillo, CCarpintero, MDiego, JEBarberis, MGarcia-Cerrada, SSoriano, JFAntonysamy, SAtwell, SMacEwan, ICondon, BSougias, CWang, JZhang, AConners, KGroshong, CWasserman, SRKoss, JWWitkin, JMLi, XOvershiner, CWafford, KASeidel, WWang, XSHeinz, BASwanson, SCatlow, JTBedwell, DWMonn, JAMitch, CHOrnstein, PL Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity. J Med Chem 59:10974-10993 (2016) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 6
Synonyms:
GPRC1F | GRM6 | GRM6_HUMAN | MGLUR6 | Metabotropic glutamate receptor 6 | glutamate receptor, metabotropic 6 precursor | metabotropic glutamate 6
Type:
Enzyme Catalytic Domain
Mol. Mass.:
95479.26
Organism:
Homo sapiens (Human)
Description:
metabotropic glutamate 6 GRM6 HUMAN::O15303
Residue:
877
Sequence:
MARPRRAREPLLVALLPLAWLAQAGLARAAGSVRLAGGLTLGGLFPVHARGAAGRACGQLKKEQGVHRLEAMLYALDRVNADPELLPGVRLGARLLDTCSRDTYALEQALSFVQALIRGRGDGDEVGVRCPGGVPPLRPAPPERVVAVVGASASSVSIMVANVLRLFAIPQISYASTAPELSDSTRYDFFSRVVPPDSYQAQAMVDIVRALGWNYVSTLASEGNYGESGVEAFVQISREAGGVCIAQSIKIPREPKPGEFSKVIRRLMETPNARGIIIFANEDDIRRVLEAARQANLTGHFLWVGSDSWGAKTSPILSLEDVAVGAITILPKRASIDGFDQYFMTRSLENNRRNIWFAEFWEENFNCKLTSSGTQSDDSTRKCTGEERIGRDSTYEQEGKVQFVIDAVYAIAHALHSMHQALCPGHTGLCPAMEPTDGRMLLQYIRAVRFNGSAGTPVMFNENGDAPGRYDIFQYQATNGSASSGGYQAVGQWAETLRLDVEALQWSGDPHEVPSSLCSLPCGPGERKKMVKGVPCCWHCEACDGYRFQVDEFTCEACPGDMRPTPNHTGCRPTPVVRLSWSSPWAAPPLLLAVLGIVATTTVVATFVRYNNTPIVRASGRELSYVLLTGIFLIYAITFLMVAEPGAAVCAARRLFLGLGTTLSYSALLTKTNRIYRIFEQGKRSVTPPPFISPTSQLVITFSLTSLQVVGMIAWLGARPPHSVIDYEEQRTVDPEQARGVLKCDMSDLSLIGCLGYSLLLMVTCTVYAIKARGVPETFNEAKPIGFTMYTTCIIWLAFVPIFFGTAQSAEKIYIQTTTLTVSLSLSASVSLGMLYVPKTYVILFHPEQNVQKRKRSLKATSTVAAPPKGEDAEAHK
  
Inhibitor
Name:
BDBM50558766
Synonyms:
CHEMBL4751065
Type:
Small organic molecule
Emp. Form.:
C15H16ClF2NO5S
Mol. Mass.:
395.806
SMILES:
Cl.[H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)([C@H](CSc1ccc(F)c(F)c1)[C@H]2O)C(O)=O |r|
Structure:
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