Table 1.

Inhibition of MMP9 by GS-5745

	Km	kcat-appa	IC50	Inhibition	α	KD
	nm		nm	%		nm
MMP9-MYC-His6						≤0.043b
MMP9-pro-cat						≤0.008b
MMP9-MYC-His6 APMA	9.6 ± 0.1	55.3 ± 1.0	0.26 ± 0.02	56 ± 2	1.2 ± 0.0	2.0 ± 0.3
MMP9-pro-catAPMA	880 ± 160	3.1 ± 0.3	0.32 ± 0.01	88 ± 8	NDc	6.6 ± 1.3
MMP9-cat	710 ± 70	5.3 ± 0.1	1.3 ± 0.1	73 ± 0	1.1 ± 0.2	3.3 ± 0.6

^ak_cat-app (relative fluorescence units × min⁻¹ × nm⁻¹) is defined as V_max/[E_tot].

^bDissociation rates were below the limit of detection and could only be estimated at ≤10⁻⁵ s⁻¹.

^cα value for competitive inhibition could not be determined due to the low activity of MMP9-pro-cat_APMA.