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Target
Excitatory amino acid transporter 1
Ligand
BDBM17657
Substrate
n/a
Meas. Tech.
ChEMBL_1735430 (CHEMBL4150966)
IC50
11482±n/a nM
Citation
 Fu, H; Zhang, J; Tepper, PG; Bunch, L; Jensen, AA; Poelarends, GJ Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors. J Med Chem 61:7741-7753 (2018) [PubMed]  Article 
Target
Name:
Excitatory amino acid transporter 1
Synonyms:
EAA1_HUMAN | EAAT1 | Excitatory Amino Acid EAAT1 | GLAST | GLAST1 | SLC1A3
Type:
Enzyme Catalytic Domain
Mol. Mass.:
59577.19
Organism:
Homo sapiens (Human)
Description:
Excitatory Amino Acid EAAT1 0 HUMAN::P43003
Residue:
542
Sequence:
MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIVGTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMGMRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPPNLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNGVNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGKIVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITALGTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFELNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRTTTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSETKM
  
Inhibitor
Name:
BDBM17657
Synonyms:
(2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutamate | Glutamate | L-Glu | L-Glutamate | L-Glutamic acid | L-[14C(U)]glutamate | L-gluatmate
Type:
Amino Acid
Emp. Form.:
C5H9NO4
Mol. Mass.:
147.1293
SMILES:
N[C@@H](CCC(O)=O)C(O)=O
Structure:
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