Table 1. Inhibitory Activity of Derivatives 1–6 on PARP1/2 and TNKS1/2.

	IC50 (nM)a
Compd	PARP-1	PARP-2	TNKS1	TNKS2
MC2050	9.3 ± 0.09	549 ± 12	218 ± 8	193 ± 7
1	2040 ± 61	340 ± 11	673 ± 28	588 ± 19
2	1480 ± 58	370 ± 8	37.4 ± 0.4	11.7 ± 0.3
3	1280 ± 49	347 ± 13	552 ± 18	103 ± 4
4	356 ± 14	963 ± 39	398 ± 14	318 ± 13
5	89.6 ± 2.2	37.8 ± 1.1	6.1 ± 0.07	0.3 ± 0.005
6	26% inhib. (@200 μM)	132000 ± 987	NIb (@200 μM)	NI (@200 μM)
PJ34	9.1 ± 0.09	14.7 ± 0.4	39.2 ± 0.9	52.7 ± 1.2
IWR-1	NI (@200 μM)	NI (@200 μM)	303 ± 9	29.2 ± 0.8

^aValues are means ± SD determined from at least two independent experiments, each one done in triplicate.

^bNI, no inhibition.