. Author manuscript; available in PMC: 2020 Jul 24.

Published in final edited form as: J Med Chem. 2019 May 24;62(11):5330–5357. doi: 10.1021/acs.jmedchem.8b01709

Table 5.

Inhibition Data for Compounds 81, 99 and 103 against PARP-Isoforms

Compd	PARP-1 IC₅₀ (nM) ^a	PARP-2 IC₅₀ (nM) ^a	TNKS1 IC₅₀ (nM) ^a	TNKS2 IC₅₀ (nM) ^a
81	30	2	>1000^b	>1000^b
99	4	0.7	6.3	8.8
103	18	4	131	198
Olaparib	1.2	0.5	NT	NT
XAV939	NT	NT	4.2	2.1

Data shown are mean values obtained from two independent experiments performed in duplicates.

% inhibition of 81 was 5% and 16% at 1000 nM for TNKS1 and TNKS2, respectively.