TABLE 1.

Summary of in vitro potency, affinity, and cooperativity parameters for N-aryl piperazine PAMs

	mGlu5-low (Ca2+)					mGlu5-high (Ca2+)		mGlu5-low (pERK1/2)
	pEC50a	pKBb,c	Logαβb,c	pKBb,d	logβd	pKBb d	logβd	pKBb,d	logβd
DPFE	6.92 ± 0.15 (0.12 μM)	5.32 ± 0.08 (4.8 μM)	1.12 ± 0.11	5.33 ± 0.07 (4.7 μM)	1.14 ± 0.05	5.99 ± 0.12 (1.0 μM)	0.94 ± 0.09	6.87 ± 0.09 (135 nM)	0.12 ± 0.02
VU0364289	6.35 ± 0.12e (0.45 μM)	5.18f (6.6 μM)	0.97f	5.22f (6.0 μM)	0.90#	5.83f (1.5 μM)	0.78f	6.29f (513 nM)	0.16f

^aNegative logarithm of the EC₅₀.

^bModulator affinity and cooperativity estimates derived using eq. 2, where a composite cooperativity parameter (logαβ) is derived.

^cNegative logarithm of the allosteric modulator equilibrium dissociation constant.

^dModulator affinity and efficacy cooperativity (β) estimate derived using eq. 1, with the assumption that α = 1.

^eVU0364289 potency previously reported in Gregory et al., 2012.

^fData from Gregory et al, 2012; provided here for benefit of comparison.