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Target
Excitatory amino acid transporter 1
Ligand
BDBM50293000
Substrate
n/a
Meas. Tech.
ChEMBL_496042 (CHEMBL998472)
IC50
4300±n/a nM
Citation
 Jensen, AA; Erichsen, MN; Nielsen, CW; Stensbøl, TB; Kehler, J; Bunch, L Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J Med Chem 52:912-5 (2009) [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:
BDBM50293000
Synonyms:
2-amino-4-(4-(2-chloro-6-fluorobenzyloxy)-3-methoxyphenyl)-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile | CHEMBL515704
Type:
Small organic molecule
Emp. Form.:
C30H24ClFN2O4
Mol. Mass.:
530.974
SMILES:
COc1cc(ccc1OCc1c(F)cccc1Cl)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1ccccc1 |c:27|
Structure:
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