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Target
Excitatory amino acid transporter 1
Ligand
BDBM50247191
Substrate
n/a
Meas. Tech.
ChEMBL_2076002 (CHEMBL4731536)
IC50
1175±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 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:
BDBM50247191
Synonyms:
(2S,3S)-2-Amino-3-benzyloxy-succinic acid | CHEMBL475341 | D,L-threo-beta-benzyloxyaspartate | DL-2-amino-3-(benzyloxy)succinic acid | DL-threo-beta-benzyloxyaspartate
Type:
Small organic molecule
Emp. Form.:
C11H13NO5
Mol. Mass.:
239.2246
SMILES:
NC(C(OCc1ccccc1)C(O)=O)C(O)=O
Structure:
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