Table 1. Binding affinities of mGlu₅ allosteric ligands derived from inhibition of [³H]methoxy-PEPy binding in intact and adherent HEK293A-rat mGlu₅-low cells and mouse cortical neurons.

Data represent mean ± SEM of 3–6 independent experiments performed in duplicate.

	HEK293A-rat mGlu5-low pKB				Mouse cortical neurons pKB
	High	Low	Fraction High	Logα	High	Low	Fraction High	Logα
MPEP	8.26 ±0.23	6.25 ±0.11	0.62 ±0.11	n.a.	8.38 ±0.30	5.92 ±0.20	0.73 ±0.11	n.a.
fenobam	7.15 ±0.28	4.66 ±0.22	0.71 ±0.09	n.a.	7.53 ±0.37a	n.a.	1a	−0.66 ±0.10
VU0409106	7.47 ±0.07	n.a.	1	−1.12 ±0.12	7.48 ±0.15	n.a.	1	−0.78 ±0.13
VU0366248	6.94 ±0.13	n.a.	1	−0.77 ±0.06	6.72 ±0.06	n.a.	1	−0.54 ±0.06
VU0366058	7.26 ±0.10	n.a.	1b	−0.82 ±0.07	6.76 ±0.23	n.a.	1b	−0.71 ±0.07
M-5MPEP	7.13 ±0.07	n.a.	1	n.a.	6.43 ±0.25	n.a.	1	n.a.
dipraglurant	7.31 ±0.11	n.a.	1	−1.24 ±0.17	6.98 ±0.14	n.a.	1	−0.89 ±0.08
MTEP	7.20 ±0.28	5.45 ±0.30	0.83 ±0.04	n.a.	8.16 ±0.14*	6.09 ±0.45	0.74 ±0.04	n.a.

^aOne individual experiment (from n=6) was best fitted to a two-site binding curve (F test p>0.05).

^bTwo individual experiments (from n=5–6) were best fitted to a two-site binding curve.

^*Denotes p<0.05, One-way ANOVA, Sidak’s multiple comparisons test, compared to HEK293A-rat mGlu₅-low

n.a. not applicable due to one-site or competitive binding curve fit