Reaction Details Report a problem with these data
Target
Excitatory amino acid transporter 1
Ligand
BDBM50292989
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:
Homo sapiens (Human)
Description:
Excitatory Amino Acid EAAT1 0 HUMAN::P43003
Residue:
542
Sequence:
MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIVGTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMGMRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPPNLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNGVNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGKIVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITALGTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFELNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRTTTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSETKM
  
Inhibitor
Name:
BDBM50292989
Synonyms:
2-Amino-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile | CHEMBL473867
Type:
Small organic molecule
Emp. Form.:
C16H14N2O2
Mol. Mass.:
266.2946
SMILES:
N=C1OC2=C(CC1C#N)C(=O)CC(C2)c1ccccc1 |c:3|
Structure:
Search PDB for entries with ligand similarity: