29: Merck90	30: Merck91	31: Bristol-Myers Squibb92	32: Bristol-Myers Squibb93
hNaV1.1 IC50	9000 nMc,i	—	—	—
hNaV1.5 IC50	>33 000 nMc,i	>34 000 nMe,p	1900 nMc,o	6400 nMc,o
hNaV1.7 IC50	66 nMe,i	87 nMe,p	4.0 nMe,j	78 nMe,f
Mouse NaV1.7 IC50	295 nM (rhesus)e,i	8800 nMe,p	7.5 nMe,j	54 nMe,f, 34 nMq
		310 nM (rhesus)e,p
Mouse PPBb	92.63% (rhesus)	94%, 98% (rhesus)	92%	97.7%, 90%r
NaV1.7 coverage in plasma@efficacious dosagea	12-Fold, 42-fold@12.06, 24.12 mg kg−1 (i.v., rhesus OB)	0.04-Fold@in vivo EC90 (mouse formalin)	>43-Fold@100 mg kg−1	14-Fold@100 mg kg−1 (mouse CCI)
	1.9-Fold@20 mg kg−1 (s.c., thermal stimulus in rhesus)	4.8-Fold@19.2 mg kg−1 (rhesus OB)	>0.77-Fold@100 mg kg−1l (mouse formalin)	0.5-Fold, 1-fold@30, 60 mg kg−1 (mouse CFA)
				3-Fold@30 mg kg−1
				1-Fold@30 mg kg−1m (mouse formalin)

^aNa_V1.7 coverage = free plasma concentration/in vitro Na_V1.7 IC₅₀.

^bPlasma protein binding.

^cValue in the automated patch-clamp assay.

^dValue in an inactivated state.

^eValue in the manual patch-clamp assay.

^fValue at V_hold = −60 mV.

^gCalculated from C_max of the PK study.

^hValue at a voltage yielding 20−50% channel inactivation.

ⁱValue at a voltage yielding approximately 20% channel inactivation.

^jValue at V_hold = −70 mV.

^kIC₅₀ of mouse DRG Na_V1.7.

^lThe target coverage in the DRG given the plasma protein binding as an estimate of tissue binding.

^mNa_V1.7 coverage in the DRG: free DRG concentration/in vitro IC₅₀ of mouse DRG Na_V1.7.

ⁿ5-Hz use-dependent voltage protocol.

^oValue at V_hold = −50 mV.

^pValue under a hyperpolarised assay protocol.

^qIC₅₀ of TTX-S currents in the mouse DRG.

^rValue of the mouse DRG.