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TargetExcitatory amino acid transporter 1
LigandBDBM50292990
Substrate/Competitorn/a
Meas. Tech.ChEMBL_665667
IC50 9200±n/a nM
Citation Erichsen, MNHuynh, THAbrahamsen, BBastlund, JFBundgaard, CMonrad, OBekker-Jensen, ANielsen, CWFrydenvang, KJensen, AABunch, L Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J Med Chem53:7180-91 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Excitatory amino acid transporter 1
Name:Excitatory amino acid transporter 1
Synonyms:Excitatory Amino Acid EAAT1
Type:Enzyme Catalytic Domain
Mol. Mass.:59577.19
Organism:Homo sapiens (Human)
Description:Excitatory Amino Acid EAAT1 0 HUMAN::P43003
Residue:542
Sequence:
MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIV
GTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMG
MRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPP
NLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNG
VNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGK
IVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITAL
GTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFE
LNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRT
TTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSET
KM
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50292990
NameBDBM50292990
Synonyms:2-amino-4-methyl-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile | CHEMBL474063
TypeSmall organic molecule
Emp. Form.C17H16N2O2
Mol. Mass.280.3211
SMILESCC1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1ccccc1 |c:8|
Structure
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n/a