Table 1.

In vitro and bio-efficacy of synthesized inhibitors

Compound name	ERAP1	ERAP1	Mouse ERAAP	ERAP2	IRAP	HeLa cells	CT26 cells
	IC50, nM*	IC50, nM†	IC50, nM*	IC50, nM*	IC50, nM*	ED50, μM	ED50, μM
DG002A [R,S]	520 ± 75	403 ± 71	650 ± 148	547 ± 110	218 ± 37	1.9 ± 1.1	0.626 ± 0.053
DG002B [R,R]	513 ± 51	481 ± 98	872 ± 137	571 ± 95	344 ± 68	ND‡	1.2 ± 0.2
DG013A [R,S,S]	33 ± 5	55.7 ± 5.8	69 ± 13	11 ± 2	30 ± 4	0.44 ± 0.16	0.033 ± 0.015
DG013B [R,R,S]	3,600 ± 500	1,574 ± 754	1,333 ± 451	1,700 ± 200	2,200 ± 300	>100	32 ± 19

^*X-AMC substrate.

^†10-mer substrate.

^‡Not determined.