Table 1.

Physicochemical characteristics of UCPH-101 and five analogs and their functional properties at EAAT1-HEK293 cells in the [³H]-d-Asp uptake assay and in the preincubation experiments. The logP values (octanol/water) and total polar surface area (tPSA) were calculated in MOE. IC₅₀ values obtained for the inhibitors in the [³H]-d-Asp uptake assay and in the preincubation experiments are given in μm with pIC₅₀ ± SEM values in parentheses

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et al., 2010) and 1 (M.N. Erichsen, J. Hansen, B. Abrahamsen, T.H.V. Huynh, C.S. Demmer, A.A. Jensen, and L. Bunch, unpublished observations).