. 2021 Aug 4;12(16):3073–3100. doi: 10.1021/acschemneuro.1c00351

Table 3. Inhibitory Potencies (pIC₅₀ ± SEM) toward mGAT1–4 Determined from the [³H]GABA Uptake Experiments and mGAT1 Binding Affinities (pK_i ± SEM) from the MS Binding Assays of the Obtained Compounds.

2.2.

			pIC₅₀ ^a ± SEM				pK_i ^a ± SEM
compd	R¹	R²	mGAT1	mGAT2	mGAT3	mGAT4	mGAT1
71	–CH₂CH₃	B	100 μM: 52%	100 μM: 54%	4.66	4.20	100 μM: 103%
72	–CH₂Ph	B	100 μM: 98%	100 μM: 63%	100 μM: 86%	100 μM: 97%	100 μM: 109%
73	–CH₂CH₃	G	100 μM: 55%	100 μM: 52%	4.6	4.28	100 μM: 94%
74	H	G	100 μM: 55%	100 μM: 55%	100 μM: 62%	100 μM: 77%	4.54
75	H	B	100 μM: 71%	100 μM: 59%	100 μM: 52%	100 μM: 60%	100 μM: 81%
tiagabine (5)¹⁹			6.88 ± 0.12	100 μM: 52%	100 μM: 64%	100 μM: 73%	7.43 ± 0.11 ⁵¹
(S)-SNAP-5114 (3)¹⁹			4.07 ± 0.09	100 μM: 56%	5.29 ± 0.04	5.81 ± 0.10	nd
DDPM-859 (4)²²			4.19 ± 0.07	4.12 ± 0.08	4.85 ± 0.04	5.78 ± 0.03	nd
DDPM-2571 (5)²⁰			8.27 ± 0.03	4.31	4.35	4.07	8.29 ± 0.02
13(25)			4.86 ± 0.10	4.98 ± 0.05	5.31 ± 0.04	5.24 ± 0.05	100 μM: 77%

Data are given as the mean ± SEM of three independent experiments that were performed in triplicate. The results presented as a percent represent [³H]GABA uptake or NO711 binding in the presence of 100 μM inhibitor. Data without the SEM imply that only one experiment was performed in triplicate. nd: not determined.

Table 3. Inhibitory Potencies (pIC50 ± SEM) toward mGAT1–4 Determined from the [3H]GABA Uptake Experiments and mGAT1 Binding Affinities (pKi ± SEM) from the MS Binding Assays of the Obtained Compounds.

Table 3. Inhibitory Potencies (pIC₅₀ ± SEM) toward mGAT1–4 Determined from the [³H]GABA Uptake Experiments and mGAT1 Binding Affinities (pK_i ± SEM) from the MS Binding Assays of the Obtained Compounds.