Table 1. Functional Properties Displayed by l-Glu, dl-TBOA, and 15a–d at hEAAT1-HEK293, hEAAT2-HEK293, hEAAT3-HEK293, and rEAAT4-tsA201 Cell Lines in the [3H]-d-Aspartate Uptake Assaye.
IFDScore of the compound pose shown in the table was the one with the highest overlay quality like the reference ligand TFB-TBOA of EAAT1cryst complex (PDB: 5mju).
IC50 values were estimate from fitted concentration-inhibition curves that were not fully completed in the concentration ranges tested (up to 300 μM).
The purity of compound 15c tested was 80%.
IC50 values are given in μM with pIC50 ± S.E.M. values in brackets, and all data are based on 3 independent experiments (n = 3).