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Target
Excitatory amino acid transporter 1
Ligand
BDBM50252048
Substrate
n/a
Meas. Tech.
ChEMBL_487931 (CHEMBL1016585)
IC50
1000000±n/a nM
Citation
 Sagot, E; Jensen, AA; Pickering, DS; Pu, X; Umberti, M; Stensbøl, TB; Nielsen, B; Assaf, Z; Aboab, B; Bolte, J; Gefflaut, T; Bunch, L Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2. J Med Chem 51:4085-92 (2008) [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:
BDBM50252048
Synonyms:
(2S,4R)-2-amino-4-(3-methoxy-3-oxopropyl)pentanedioic acid | (2S,4R)-4-(3-Methoxy-3-oxopropyl)glutamic Acid | CHEMBL482080
Type:
Small organic molecule
Emp. Form.:
C9H15NO6
Mol. Mass.:
233.2185
SMILES:
COC(=O)CC[C@H](C[C@H](N)C(O)=O)C(O)=O |r|
Structure:
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