Table 1.

Inhibitory constants (nM) for acyclic compounds vs human MTAP and bacterial MTANs

Compound	Ki human MTAPa nM	Ki E. coli MTANa nM	Ki N. men. MTANa nM
3	1.0 ± 0.5b,c	0.08 ± 0.02d	0.36e
4	0.09 ± 0.01c	0.002 ± .0002d	0.14e
17 III	12 ± 1	1.7 ± 0.2	0.80 ± .06
17 I	4.4 ± 0.2	0.23 ± 0.2	NDf
17 II	34 ± 3	1.1 ± 0.4	NDf
(±)-25	10 ± 1	0.36 ± 0.04	1.2 ± 0.1
33	5.2 ± 0.4	0.8 ± 0.1	0.9 ± 0.1
ent-33	87 ± 11	3.9 ± 0.5	6 ± 1
40	87 ± 8	10 ± 2	10 ± 1
ent-40	34 ± 18	2.1 ± 0.5	1.8 ± 0.4
47	34 ± 24	5.8 ± 0.8	4 ± 2
54	602 ± 83	40 ± 5	36 ± 4
(±)-65	34 ± 6	9 ± 2	5 ± 1
(±)-68	12 ± 2	2300 ± 600	61 ± 5
(±)-72	105 ± 30	401 ± 37	132 ± 9
(±)-78	368 ± 153	202 ± 35	85 ± 6
79	130 ± 20	1720 ± 850	47 ± 4

^afor compounds 3 and 4 these are K_i* values;

^bRef 34;

^cRef 35;

^dRef 44;

^eRef 40;

^fND – not determined