Table 1.

Kinetics of PARP1 inhibitor binding to PARP1 and TNKS1^a,b

Inhibitor	PARP1				TNKS1
	kon (M−1 s−1)	koff (s−1)	t1/2 (min)	Kin. KD (nM)	kon (M−1 s−1)	koff (s−1)	t1/2 (min)	Kin. KD (nM)
Talazoparib	1.3 × 105	7.3 × 10−5	158	0.6 ± 0.1	1.8 × 105	2.6 × 10−3	4	14 ± 1
Olaparib	1.1 × 105	8.8 × 10−5	131	0.8 ± 0.1	1.1 × 105	1.7 × 10−1	0.1	1700 ± 6
Veliparib	7.5 × 105	3.6 × 10−3	5	6.2 ± 3.5	3.1 × 103	5.4 × 10−2	0.2	17,500 ± 300
Niraparib	3.4 × 105	1.7 × 10−3	7	5.4 ± 1.4	2.5 × 104	8.3 × 10−1	0.01	34,800 ± 540

^aBinding kinetics measured in 25 mM Hepes, 150 mM NaCl, 5% glycerol, 0.5 mM TCEP, 2% DMSO, 0.02% Tween 20, and pH 7.4, at 25 °C.

^bEach value in the table represents an average of two or more independent measurements.