Table 2.
Estimation of concentrations for specific binding of compounds classified as hits in the deliberately compiled 128 compound library based on RRFs.
| Sublibrary | GAT1 inhibitor | Specific binding (nM) | pKi |
|---|---|---|---|
| A | DDPM2330 | 0.72 | 7.15 |
| DDPM2565 | 10.0 | 7.83 | |
| Telmisartan | 1.58 | n.d. | |
| B | DDPM3138 | 1.90 | 7.81 |
| DDPM2188 | 0.38 | 6.42 | |
| Pilocarpine | 0.24 | n.d. | |
| C | DDPM2077 | 0.48 | 5.94 |
| DDPM2029 | 3.18 | 6.32 | |
| D | DDPM2187 | 0.22 | 6.50 |
| DDPM2473 | 3.44 | 8.13 | |
| E | DDPM1981 | 2.20 | 7.04 |
| DDPM1349 | 0.20 | 6.40 | |
| F | DDPM2009 | 2.95 | 6.16 |
| G | Trifluoperazine | 1.46 | n.d. |
n.d., pKi value unavailable.