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Target
Excitatory amino acid transporter 1
Ligand
BDBM50197050
Substrate
n/a
Meas. Tech.
ChEMBL_1619055 (CHEMBL3861224)
IC50
2512±n/a nM
Citation
 Hansen, JC; Bjørn-Yoshimoto, WE; Bisballe, N; Nielsen, B; Jensen, AA; Bunch, L ß-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences. J Med Chem 59:8771-8786 (2016) [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:
BDBM50197050
Synonyms:
CHEMBL3920886
Type:
Small organic molecule
Emp. Form.:
C10H9F3N2O6S
Mol. Mass.:
342.248
SMILES:
N[C@@H](C(NS(=O)(=O)c1cc(F)c(F)cc1F)C(O)=O)C(O)=O |r|
Structure:
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