Table 3.

Kinetic parameters of compounds tested against main carbapenemases.

Inhibitor		Clinically Most Relevant Carbapenemases
		KPC-2	IMP-1	VIM-1	NDM-1	OXA-23	OXA-24/40	OXA-48
Diazabicyclooctane-derived
Avibactam	IC50 (nM)	170 [30] */22 [31]/60 [32]	>1.6 × 105 [31]/>1.0 × 105 [32]	>1.6 × 105 [31]	>1.6 × 105 [31]/>1.0 × 105 [32]	3.1 × 103 [31]/8.9 × 103 [33]	1.60 × 104 [30]/2.23 × 104 [33]	180 [31]/550 [32]
	Kiapp (nM)	900 [34]/11 [35]	>4.0 × 104 [35]	>4.0 × 104 [35]	>4.0 × 104 [35]	>1.0 × 105 [34]/1.7 × 103 [35]	>1.0 × 105 [34]/1.54 × 105 [33]	3.0 × 104 [34]/27 [35]
Relebactam	IC50 (nM)	82 [31]/230 [36]	>1.6 × 105 [31]	>1.6 × 105 [31]	>1.6 × 105 [31]			9 × 104 [31]
	Kiapp (nM)	2.2 × 103 [34]/1.2 × 103 [36]				>1.0 × 105 [34]	>1.0 × 105 [34]	>1.0 × 105 [34]
Zidebactam	IC50 (nM)
	Kiapp (nM)	4.5 × 103 [34]		>1.00 × 105 (VIM-2) [37]		>1.0 × 105 [34]	>1.0 × 105 [34]	>1.0 × 105 [34]
Durlobactam	IC50 (nM)	4 [30]					190 [30]
	Kiapp (nM)
Nacubactam	IC50 (nM)	869 [38]	>3.0 × 105 [38]			4.64 × 104 [38]
	Kiapp (nM)	3.1 × 104 [39]
ETX1317	IC50 (nM)	43 [40]					540 [40]	77 [40]
	Kiapp (nM)
WCK 4234	IC50 (nM)
	Kiapp (nM)	320 [34]				8.0 × 103 [34]	5.0 × 103 [34]	290 [34]
Boronic acid-derived
Vaborbactam	IC50 (nM)	110 [31]/100 [32]	>1.6 × 105 [31]/>1.0 × 105 [32]	>1.6 × 105 [31]	>1.6 × 105 [31]/>1.0 × 105 [32]	1.2 × 105 [31]		6.9 × 103 [31]/3.88 × 104 [32]
	Kiapp (nM)	22 [41]/56 [35]	>3.0 × 104 [41]/>4.0 × 104 [35]	>4.0 × 104 [35]	>3.0 × 104 [41]/>4.0 × 104 [35]	>4.0 × 104 [35]		350 [41]/1.4 × 104 [35]
Taniborbactam	IC50 (nM)	30 [32]	2.51 × 103 [42]/3.98 × 104 [32]	7.9 [42]	10 [42]/190 [32]			537 [42]/420 [32]
	Kiapp (nM)	4 [41]	>3.0 × 104 [41]	19 (VIM-2) [41]	81 [41]			350 [41]
VNRX-5236	IC50 (nM)	80 [43]	>1.0 × 105 [43]	9.04 × 103 (VIM-2) [43]	3.81 × 104 [43]			317 [43]
	Kiapp (nM)	110 [43]
QPX7728	IC50 (nM)	2.9 [31]	610 [31]	14 [31]	55 [31]	1.2 [31]		1.1 [31]
	Kiapp (nM)	1.9 [35]	220 [35]	8 [35]	32 [35]	0.74 [35]		0.28 [35]
β-lactam-derived
Enmetazobactam	IC50 (nM)	360 a [44]						1.1 × 104 a [44]
	Kiapp (nM)
LN-1-255	IC50 (nM)					12 [33]	15 [33]	3 [45]
	Kiapp (nM)					88 [33]	289 [33]	170 [45]
Pyridine-2-carboxylic acid
ANT2681	IC50 (nM)
	Kiapp (nM)		3.81 × 103 [46]	630 [46]	40 [46]

^a Assays performed with bacterial extracts, not purified enzyme. * Numbers in brackets corresponde with references.