Table 4.

Inhibition potency and ligand efficiency of compounds towards the OXA-48, OXA-24 and OXA-58 carbapenemases.

	OXA-48		OXA-24		OXA-58
compound	Ki (μM)	LEa	Ki (μM)	LE	Ki (μM)	LE
2.1	15 ± 1	0.37	87 ± 3	0.31	12.9 ± 0.1	0.37
2.2	4.3 ± 0.1	0.41	70 ± 3	0.32	1.8 ± 0.1	0.44
2.3	1.7 ± 0.1	0.44	118.4 ± 0.9	0.30	45.8 ± 0.6	0.33
3.1	5.1 ± 0.1	0.40	150 ± 6	0.29	120 ± 5	0.30
3.2	50.0 ± 0.5	0.29	520 ± 33	0.22	410 ± 1	0.23
3.3	11.7 ± 0.8	0.34	140 ± 7	0.26	30 ± 2	0.31
3.4	267 ± 19	0.27	3200 ± 18	0.19	2100 ± 260	0.20
3.5	96.7 ± 0.8	0.29	330 ± 19	0.25	500 ± 21	0.24
4.1	257 ± 8	0.31	2300 ± 250	0.23	270 ± 4	0.31
4.2	410 ± 27	0.29	>2000	N/Ab	2100 ± 170	0.23
4.3	1.36 ± 0.09	0.38	34 ± 1	0.29	3.4 ± 0.3	0.36
5.1	52 ± 2	0.31	480 ± 19	0.24	120 ± 13	0.28
5.2	76 ± 3	0.28	920 ± 23	0.21	93 ± 2	0.28
6.1	7.9 ± 0.4	0.30	7.9 ± 0.6	0.30	1.7 ± 0.1	0.34

^aLigand efficiency. Calculated as described in Methods.

^bN/A - not applicable