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Target
Excitatory amino acid transporter 2
Ligand
BDBM50327877
Substrate
n/a
Meas. Tech.
ChEMBL_664973 (CHEMBL1259930)
IC50
1400±n/a nM
Citation
 Luethi, E; Nguyen, KT; Bürzle, M; Blum, LC; Suzuki, Y; Hediger, M; Reymond, JL Identification of selective norbornane-type aspartate analogue inhibitors of the glutamate transporter 1 (GLT-1) from the chemical universe generated database (GDB). J Med Chem 53:7236-50 (2010) [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:
BDBM50327877
Synonyms:
(1R*,2R*,3S*,4R*,6R*)-2-Amino-6-phenethyl-bicyclo[2.2.1]-heptane-2,3-dicarboxylic Acid Trifluoroacetate | CHEMBL1258906
Type:
Small organic molecule
Emp. Form.:
C17H21NO4
Mol. Mass.:
303.3529
SMILES:
N[C@@]1(C2C[C@H](C[C@H]2CCc2ccccc2)[C@@H]1C(O)=O)C(O)=O |r,TLB:7:6:3:1.15,0:1:5.6:3,THB:16:15:5.6:3|
Structure:
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