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Target
Excitatory amino acid transporter 1
Ligand
BDBM50328520
Substrate
n/a
Meas. Tech.
ChEMBL_833020 (CHEMBL2067159)
IC50
>300000±n/a nM
Citation
 Huynh, TH; Shim, I; Bohr, H; Abrahamsen, B; Nielsen, B; Jensen, AA; Bunch, L Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circ J Med Chem 55:5403-12 (2012) [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:
Human
Description:
Excitatory Amino Acid EAAT1 0 HUMAN::P43003
Residue:
542
Sequence:
MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIVGTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMGMRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPPNLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNGVNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGKIVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITALGTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFELNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRTTTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSETKM
  
Inhibitor
Name:
BDBM50328520
Synonyms:
CHEMBL1259099 | syn-2-Amino-5-oxo-4,7-diphenyl-4,5,7,8-tetrahydropyrano[4,3-b]-pyran-3-carbonitrile
Type:
Small organic molecule
Emp. Form.:
C21H16N2O3
Mol. Mass.:
344.3633
SMILES:
N=C1OC2=C([C@@H](C1C#N)c1ccccc1)C(=O)O[C@H](C2)c1ccccc1 |r,c:3|
Structure:
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