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Target
Excitatory amino acid transporter 1
Ligand
BDBM50366617
Substrate
n/a
Meas. Tech.
ChEMBL_1735430 (CHEMBL4150966)
IC50
1200±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:
BDBM50366617
Synonyms:
CHEMBL4163105
Type:
Small organic molecule
Emp. Form.:
C9H11NO5S
Mol. Mass.:
245.252
SMILES:
N[C@@H]([C@H](OCc1cccs1)C(O)=O)C(O)=O |r|
Structure:
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