Table 1.
Compound | logP | tPSA | [3H]-d-Asp uptakea IC50 (μm) (pIC50 ± SEM) | Preincubation IC50 (μm) (pIC50 ± SEM) |
---|---|---|---|---|
UCPH-101 | 3.94 | 151 | 0.66 (6.18 ± 0.08) | 0.23 (6.64 ± 0.15) |
UCPH-102 | 2.71 | 156 | 0.42 (6.47 ± 0.21) | 20 (4.71 ± 0.20) |
UCPH-100 | 2.76 | 150 | 3.9 (5.48 ± 0.20) | ∼300 (∼3.5) |
1 | 3.45 | 155 | 0.87 (6.11 ± 0.15) | ∼30 (∼4.5) |
2 | 2.42 | 262 | 11 (4.97 ± 0.05) | >300 (<3.5) |
3 | 1.49 | 156 | 9.2 (5.04 ± 0.05) | >300 (<3.5) |
Results from the preincubation experiments are based on 3–4 individual experiments performed in duplicate as described in Materials and Methods and in the legend to Figure 3G.
a The IC50 values for the ligands in the [3H]-d-Asp uptake assay have been reported previously: UCPH-101, 2 and 3 (Jensen et al., 2009), UCPH-102 and UCPH-100 (Erichsen et al., 2010) and 1 (M.N. Erichsen, J. Hansen, B. Abrahamsen, T.H.V. Huynh, C.S. Demmer, A.A. Jensen, and L. Bunch, unpublished observations).