Target
Excitatory amino acid transporter 2
Ligand
BDBM50410455
Substrate
n/a
Meas. Tech.
ChEMBL_321549 (CHEMBL881963)
IC50
100±n/a nM
Citation
 Greenfield, AGrosanu, CDunlop, JMcIlvain, BCarrick, TJow, BLu, QKowal, DWilliams, JButera, J Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2. Bioorg Med Chem Lett 15:4985-8 (2005) [PubMed]  Article 
Target
Name:
Excitatory amino acid transporter 2
Synonyms:
EAA2_HUMAN | EAAT2 | GLT1 | Glutamate/aspartate transporter II | SLC1A2 | Sodium-dependent glutamate/aspartate transporter 2 | Solute carrier family 1 member 2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
62103.57
Organism:
Homo sapiens (Human)
Description:
Excitatory Amino Acid EAAT2 0 0::P43004
Residue:
574
Sequence:
MASTEGANNMPKQVEVRMHDSHLGSEEPKHRHLGLRLCDKLGKNLLLTLTVFGVILGAVCGGLLRLASPIHPDVVMLIAFPGDILMRMLKMLILPLIISSLITGLSGLDAKASGRLGTRAMVYYMSTTIIAAVLGVILVLAIHPGNPKLKKQLGPGKKNDEVSSLDAFLDLIRNLFPENLVQACFQQIQTVTKKVLVAPPPDEEANATSAVVSLLNETVTEVPEETKMVIKKGLEFKDGMNVLGLIGFFIAFGIAMGKMGDQAKLMVDFFNILNEIVMKLVIMIMWYSPLGIACLICGKIIAIKDLEVVARQLGMYMVTVIIGLIIHGGIFLPLIYFVVTRKNPFSFFAGIFQAWITALGTASSAGTLPVTFRCLEENLGIDKRVTRFVLPVGATINMDGTALYEAVAAIFIAQMNGVVLDGGQIVTVSLTATLASVGAASIPSAGLVTMLLILTAVGLPTEDISLLVAVDWLLDRMRTSVNVVGDSFGAGIVYHLSKSELDTIDSQHRVHEDIEMTKTQSIYDDMKNHRESNSNQCVYAAHNSVIVDECKVTLAANGKSADCSVEEEPWKREK
  
Inhibitor
Name:
BDBM50410455
Synonyms:
CHEMBL2113116
Type:
Small organic molecule
Emp. Form.:
C17H15ClN2O3
Mol. Mass.:
330.766
SMILES:
N[C@@H](CC(=O)Nc1ccc-2c(Cc3cc(Cl)ccc-23)c1)C(O)=O |r|
Structure:
Search PDB for entries with ligand similarity: