Table 1.

IC₅₀ values of REL-1017 and reference NMDAR blockers.

	NR1-2A			NR1-2B			NR1-2C			NR1-2D
	IC50 (µM)	Slope	Min. (%)	IC50 (µM)	Slope	Min. (%)	IC50 (µM)	Slope	Min. (%)	IC50 (µM)	Slope	Min. (%)
REL-1017	43	−1.0	30	25	−1.1	14	23	−0.84	15	68	−0.68	47
(±)-Ketamine	30	−0.76	23	6.3	−0.78	8	3.4	−0.83	8	11	−1.1	12
Memantine	34	−0.82	29	10	−0.86	11	3.6	−0.82	13	7.3	−0.88	18
Dextromethorphan	51	−0.80	35	15	−0.89	14	5.2	−1.0	14	28	−1.2	43
MK-801	0.29	−0.69	4	0.07	−0.94	4	0.58	−1.0	7	0.76	−1.2	11

IC₅₀ values of five selected NMDAR channel blockers were obtained via FLIPR assay, as exemplified for REL-1017 in Figure 1. Fitting values were obtained for every heterodimeric NMDAR via logistic equation in GraphPad Prism v8.0. Slope is also reported in the table, as well as the minimal % Ca²⁺ influx measured in the presence of 100 μM blocker, the highest tested concentration. For example, 100 μM REL-1017 reduced Ca²⁺ influx elicited by 10 μM L-glutamate by 15% in the 2C-containing cell line.