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Target
Excitatory amino acid transporter 2
Ligand
BDBM50561801
Substrate
n/a
Meas. Tech.
ChEMBL_2076003 (CHEMBL4731537)
IC50
209±n/a nM
Citation
 Liu, N; Jensen, AA; Bunch, L ?-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs). ACS Med Chem Lett 11:2212-2220 (2020) [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:
BDBM50561801
Synonyms:
CHEMBL4759043
Type:
Small organic molecule
Emp. Form.:
C26H23F3N2O9S2
Mol. Mass.:
628.594
SMILES:
OC(=O)C(F)(F)F.Cc1ccc(cc1)S(=O)(=O)n1cc(-c2ccsc2)c2ccc(CO[C@@H]([C@H](N)C(O)=O)C(O)=O)cc12 |r|
Structure:
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