Table 1.

Compounds screened for their general inhibitory potential towards PARP10 in vitro and in cells.

Comp.	X	Y	PARP10cat[a] Automod.	CFA[b]
4	C(O)NH2	C(O)OH	active	inactive
5	C(O)NH2	C(O)OMe	active	5‐10 μm
6	C(S)NH2	C(O)OMe	inactive	inactive
7	CN	C(O)NHNH2	n.a.[c]	inactive
8	C(O)NH2	C(O)NHNH2	active	inactive
9	C(S)NH2	C(O)OH	active	inactive
10	C(O)NH2	CN	active	1–2 μm
11	C(O)NH2	5‐tetrazolyl	active	inactive
12	C(S)NH2	5‐tetrazolyl	active	inactive
13	C(S)NH2	CN	active	inactive
14	C(O)OMe	5‐tetrazolyl	inactive	inactive
15	C(O)OH	5‐tetrazolyl	inactive	inactive
16	CN	CN	active	inactive
17	C(S)NH2	C(S)NH2	inactive	inactive
18	C(O)NH2	C(S)NH2	active	5–10 μm
19	CN	C(O)NH2	active	5–10 μm [d]
20	C(O)NH2	C(O)NH2	active	1–2 μm
21	C(O)NH2	C(O)OH	inactive	inactive
22	C(O)NH2	C(O)OMe	inactive	inactive
23	5‐tetrazolyl	C(O)NH2	active	inactive
24	C(S)NH2	C(O)NH2	active	inactive
25	C(O)NH2	CN	active	inactive
26	C(O)NH2	5‐tetrazolyl	active	inactive
27	C(O)NH2	C(S)NH2	active	inactive
28	CN	CN	inactive	n.a.
29	C(O)NH2	C(O)NH2	inactive	inactive
30	C(O)NH2	C(O)NH2	inactive	n.a.
31	CN	C(O)NH2	inactive	n.a.
32	C(O)NH2	C(O)OH	inactive	n.a.

[a] Automodification and analysis by SDS‐PAGE, active and inactive refers to compounds that inhibited at 10 μm or did not, respectively. Examples are shown in Figures 3 and S1 in the Supporting Information.[b] Colony‐formation assay (CFA) in HeLa‐PARP10 cells with estimated IC50 values. [c] not analyzed (n.a.). [d] Very small colonies, suggesting some toxic effect.