Table 1.

Summary of GluN2A-selective modulators.

			Activity at GluN1/2X (in μM)
Compound			2A	2B	2C	2D
NVP-AAM077		KBa	0.015	0.078	-	-	[352]
TCN-201		KBa,b	0.045 0.070 0.027	NE	NE	NE	[356] [355] [158]
MPX-004		IC50c,d	0.079c 0.198†	NEc NE†	-c NE†	NEc NE†	[357]
MPX-007		IC50c,d	0.027c 0.143†	NEc ND†	-c NE†	NEc NE†	[357]
GNE-3419		EC50c	2.03	NR	NR	NR	[157]
GNE-6901		EC50c	0.33	NR	NR	NR	[157]
GNE-0723		EC50c	0.021	ND	7.4	6.2	[170]
GNE-8324		EC50c	2.43	NR	NR	NR	[157]

^-denotes not determined, NE denotes no effect at the highest concentrations evaluated, and ND indicates that the compound displayed some activity, but the affinity or potency could not be determined. NR denotes some activity, but that the numerical affinity value was not reported. Unless otherwise stated (also denoted by ^†), the values were determined using two-electrode voltage-clamp experiments with Xenopus oocytes.

^adenotes when Schild analysis was used for affinity determination.

^bthree independent studies are published reporting the K_B of TCN-201 at GluN1/2A.

^cdenotes that potency (i.e. half maximally effective concentration) was determined using a Ca²⁺ imaging assay.

^dExperiments using MPX compounds were performed in 3 μM glycine.