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Target
Excitatory amino acid transporter 3
Ligand
BDBM86712
Substrate
n/a
Meas. Tech.
ChEMBL_1735432 (CHEMBL4150968)
IC50
1862±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 3
Synonyms:
EAA3_HUMAN | EAAC1 | EAAT3 | Excitatory Amino Acid EAAT3 | HEAAC1 | SLC1A1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
57096.71
Organism:
Homo sapiens (Human)
Description:
Excitatory Amino Acid EAAT3 0 HUMAN::P43005
Residue:
524
Sequence:
MGKPARKGCEWKRFLKNNWVLLSTVAAVVLGITTGVLVREHSNLSTLEKFYFAFPGEILMRMLKLIILPLIISSMITGVAALDSNVSGKIGLRAVVYYFCTTLIAVILGIVLVVSIKPGVTQKVGEIARTGSTPEVSTVDAMLDLIRNMFPENLVQACFQQYKTKREEVKPPSDPEMNMTEESFTAVMTTAISKNKTKEYKIVGMYSDGINVLGLIVFCLVFGLVIGKMGEKGQILVDFFNALSDATMKIVQIIMCYMPLGILFLIAGKIIEVEDWEIFRKLGLYMATVLTGLAIHSIVILPLIYFIVVRKNPFRFAMGMAQALLTALMISSSSATLPVTFRCAEENNQVDKRITRFVLPVGATINMDGTALYEAVAAVFIAQLNDLDLGIGQIITISITATSASIGAAGVPQAGLVTMVIVLSAVGLPAEDVTLIIAVDWLLDRFRTMVNVLGDAFGTGIVEKLSKKELEQMDVSSEVNIVNPFALESTILDNEDSDTKKSYVNGGFAVDKSDTISFTQTSQF
  
Inhibitor
Name:
BDBM86712
Synonyms:
CAS_868359-05-1 | N-[4-(2-BROMO-4,5-DIFLUOROPHENOXY)PHENYL]-L-ASPARAGINE | WAY 213613
Type:
Small organic molecule
Emp. Form.:
C16H13BrF2N2O4
Mol. Mass.:
415.186
SMILES:
N[C@@H](CC(=O)Nc1ccc(Oc2cc(F)c(F)cc2Br)cc1)C(O)=O |r|
Structure:
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