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. Author manuscript; available in PMC: 2018 May 4.
Published in final edited form as: J Med Chem. 2016 Dec 21;60(4):1262–1271. doi: 10.1021/acs.jmedchem.6b00990

Table 2.

In Vitro Potencies of PARP Inhibitorsa

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Veliparib Niraparib Olaparib Talazoparib Rucaparib PJ34 1 (UPF1069)
Protein Construct pIC50 IC50 pIC50 IC50 pIC50 IC50 pIC50 IC50 pIC50 IC50 pIC50 IC50 pIC50 IC50
PARP1 FL 8.48±0.14 3.3 7.79±0.08 16.7 8.86±0.12 1.4 8.95±0.18 1.1 8.50±0.08 3.2 7.96±0.10 10.9 6.84±0.68 145
PARP1 Zn3-C 6.45±0.07 354 7.16±0.10 18.9 6.52±0.08 301 6.32±0.07 481
PARP1 ART 7.45±0.08 35.2 6.88±0.14 132 7.99±0.07 10 7.40±0.12 39.8 7.22±0.13 61
PARP2 FL 7.76±0.10 17.5 7.81±0.16 15.3 7.91±0.11 12.3 8.38±0.06 4.1 7.55±0.18 28.2 7.48±0.06 33.5 5.97±0.05 1000
PARP2 ART 6.86±0.07 137 6.60±0.12 251 6.86±0.09 138 6.42±0.06 382
PARP3 FL 5.67±0.11 2040 6.53±0.18 296 6.64±0.10 230 7.20±0.04 62.8 6.39±0.09 512 5.84±0.15 1430 5.89±0.21 1300
PARP4 ART 5.46±0.09 3500 6.35±0.14 446 6.39±0.11 410 6.59±0.14 254 6.08±0.09 839 6.12±0.18
TNKS1 SAM-ART 4.97±0.06 10740 6.49±0.13 322 6.84±0.05 144 5.51±0.12 3100
TNKS1 ART 5.63±0.08 2355 5.91±0.06 1230 5.77±0.05 1690
TNKS2 ART 4.62±0.10 24000 5.29±0.96 5130 5.3±0.04 2340 6.97±0.07 108 6.05±0.05 890 5.53±0.10 2900
PARP10 FL 5.72±0.15 1900 5.71±0.07 1900 5.03±0.09 9300 5.11±0.08 7800 6.25±0.11 570 5.23±0.10 5800 5.15±0.08 7100
PARP10 ART 4.36±0.07 43800 5.48±0.04 3300 5.90±0.07 1250 5.64±0.05 2310 5.17±0.15 6800
PARP12 ART 4.23±0.27 59400 6.10±0.15 79 4.99±0.04 10050 5.18±0.15 6650 6.65±0.11 230
PARP14 ART 4.05±0.26 89000 5.76±0.08 17300 n.i. n.i. 4.60±0.04 25500 5.05±0.05 8830 5.38±0.05 4200 5.24±0.09 5700
PARP15 ART n.i. n.i. 4.54±0.16 29200 4.75±0.06 17600 4.32±0.16 47400 4.49±0.07 32600 5.05±0.15 9000
PARP16 FL n.i. n.i. 5.29±0.17 5100 5.73±0.15 1900 n.i. n.i.
a

IC50 values in nanomolar (nM)