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Target
Excitatory amino acid transporter 1
Ligand
BDBM50534104
Substrate
n/a
Meas. Tech.
ChEMBL_1927835 (CHEMBL4430907)
IC50
<316228±n/a nM
Citation
 Hansen, SW; Erichsen, MN; Fu, B; Bjørn-Yoshimoto, WE; Abrahamsen, B; Hansen, JC; Jensen, AA; Bunch, L Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study. J Med Chem 59:8757-8770 (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:
BDBM50534104
Synonyms:
CHEMBL4524413
Type:
Small organic molecule
Emp. Form.:
C21H16ClNO6S
Mol. Mass.:
445.873
SMILES:
CCOC(=O)CN1C(=O)S\C(=C/c2ccc(cc2)-c2cc(ccc2Cl)C(O)=O)C1=O
Structure:
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