| Reaction Details |
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 | Report a problem with these data |
| Target | Excitatory amino acid transporter 1 |
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| Ligand | BDBM50366616 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1735430 (CHEMBL4150966) |
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| IC50 | 5.1±n/a nM |
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| Citation |  Fu, H; Zhang, J; Tepper, PG; Bunch, L; Jensen, AA; Poelarends, GJ Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors. J Med Chem61:7741-7753 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Excitatory amino acid transporter 1 |
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| Name: | Excitatory amino acid transporter 1 |
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| Synonyms: | EAA1_HUMAN | EAAT1 | Excitatory Amino Acid EAAT1 | GLAST | GLAST1 | SLC1A3 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 59577.19 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Excitatory Amino Acid EAAT1 0 HUMAN::P43003 |
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| Residue: | 542 |
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| Sequence: | MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIV
GTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMG
MRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPP
NLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNG
VNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGK
IVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITAL
GTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFE
LNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRT
TTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSET
KM
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| BDBM50366616 |
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| n/a |
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| Name | BDBM50366616 |
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| Synonyms: | CHEMBL4176427 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H21F3N2O6 |
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| Mol. Mass. | 454.3964 |
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| SMILES | N[C@@H]([C@H](OCc1cccc(NC(=O)CCc2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| |
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| Structure | 
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