Table 1.

IC₅₀ and MIC Values^a

cmpd	IC50 (μM)	K204 MICKAN (μg/mL) with 100 μM cmpdb	H37Rv mc2 6230 (6206) MIC (μg/mL)	H37Rv mc2 6230 (6206) MIC (μM)	cmpd	IC50 (μM)	K204 MICKAN (μg/mL) with 100 μM cmpdb	H37Rv mc2 6230 (6206) MIC (μg/mL)	H37Rv mc2 6230 (6206)MIC (μM)
KAN	N/A	>10, >10d	<1	<1.72	5e	7.0 ± 0.7	10, 10	>128	>340
1a	2.2 ± 0.3	10, 10	8	25	6e	4.6 ± 0.6	toxic	4 (8)	9.9 (20)
2a	0.99 ± 0.06	5, 5	4	12	7e	0.46 ± 0.17	toxic	8	19
3a	6.7 ± 0.7	10, 10	2−4	5.7−12	8e	2.5 ± 0.1	5, toxic	32	88
4a	2.4 ± 0.2	5, 2.5, toxic	4	12	1f	11 ± 1	10, 10	>128	>363
5a	>200	NT	>128	>353	2f	1.5 ± 0.1	5, 5	>128	>350
6a	23 ± 5	toxic	4	10	3f	52 ± 7	>10, >10	>128	>337
7a	4.0 ± 1.1	toxic	4	9.7	4f	3.6 ± 0.4	10, 10	128	337
8a	6.6 ± 0.6	10, >10	4	11	5f	1.1 ± 0.1	NT	64	162
1b	1.9 ± 0.2	5, 5	64	191	6f	∼200	NT	>128	>303
2b	1.1 ± 0.1	5, 5	32	92	7f	3.0 ± 0.6	toxic	16	36
3b	14 ± 1	10, 10	32	88	8f	8.7 ± 1.2	10, 10	>100	>263
4b	2.0 ± 0.3	5, 10	8	22	1gc	1.9 ± 0.6	NT	>128	>337
5b	5.4 ± 0.5	toxic	4 (8)	11 (21)	2gc	0.25 ± 0.02	2.5, 2.5	>128	>325
6b	16 ± 2	toxic	4 (4−8)	9.9 (9.9−20)	3g	∼2.4	NT	128	314
7b	16 ± 2	10, 10	16	38	4g	0.20 ± 0.03	5, 2.5	64	157
8b	7.6 ± 1.1	toxic	32	88	5g	1.1 ± 0.2	toxic	16	38
1cc	0.75 ± 0.06	2.5, 2.5	32−64	92−183	6g	>200	NT	>128	>284
2c	0.17 ± 0.04	2.5, 2.5	64	176	7g	0.48 ± 0.06	toxic	32	68
3c	3.8 ± 0.5	5, 5, 2.5	16	42	8g	3.1 ± 0.3	5, 5	8	20
4cc	0.61 ± 0.08	toxic	16	42	1hc	2.5 ± 0.4	5, 5	>128	>327
5c	0.91 ± 0.13	toxic	16	41	2h	0.46 ± 0.06	2.5, 2.5	>128	>315
6c	6.6 ± 1.2	toxic	32	76	3h	6.8 ± 0.6	10, 10	>128	>305
7cc	0.23 ± 0.08	toxic	4 (8)	9.1 (18)	4h	3.7 ± 0.6	2.5, 2.5	64	152
8cc	1.2 ± 0.1	toxic	16	42	5hc	0.68 ± 0.09	toxic	32	74
1d	1.8 ± 0.1	5, 5	16	48	6h	10 ± 4	toxic	16	35
2d	0.45 ± 0.03	5, 5	16	46	7h	0.93 ± 0.29	toxic	8	17
3d	3.6 ± 0.2	2.5, 5	16	44	8hc	0.30 ± 0.06	NT	>128	>305
4d	0.81 ± 0.13	toxic	8	22	1i	17 ± 1	5, 5	>128	>325
5d	>200	NT	>128	>340	2ic	1.6 ± 0.2	2.5, 2.5	>128	>314
6d	6.3 ± 1.5	toxic	4 (8−16)	9.9 (20−40)	3i	56 ± 6	10, 10	>128	>303
7d	0.53 ± 0.04	NT	16	38	4i	0.47 ± 0.08	1.25, 2.5, 2.5	>100	>237
8d	2.3 ± 0.2	5, 10	16	44	5i	19 ± 3	5, 5	128	294
1e	0.80 ± 0.10	10, 5	128	382	6i	>200	toxic	32	69
2ec	0.15 ± 0.02	2.5, 2.5	64	183	7i	16 ± 3	5, toxic, toxic	32	66
3e	2.0 ± 0.1	5, 2.5, 5, 5	64	176	8i	8.5 ± 1.3	5, 5	>128	>303
4ec	0.36 ± 0.05	toxic	8	21

^aN/A = not applicable; NT = not tested.

^bMultiple MIC values are the results of independent experiments.

^cX-ray structures of Eis in complex with these inhibitors are presented in this study.

^dNote that the MIC of KAN in the parent H37Rv from which the K204 strain is derived is 1.25 μg/mL.