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. 2022 May 24;65(11):7532–7560. doi: 10.1021/acs.jmedchem.2c00281

Table 2. Selectivity Profile of OUL35 (3) and Its Analogues against a Panel of ARTs (μM IC50s) and Activity in the Cell-Based Assay (μM).

  OUL35 (3)a 8b 9b 10c 11c 12d 15d 16d 17d 18e
PARP10 0.330 0.230 2.4 3.64 0.480 0.290 0.140 0.150 0.160 0.400
PARP15 >10f 3.3 1.2 11.0 1.7 2.4 0.400 0.400 0.370 n.t.g
PARP14 23 10 0.630 >100 41 ≫10 ≫10 ≫10 ≫10 5.2
TNKS1 >100 >100 n.t. >100 21 >100 >100 >100 >100 n.t.
TNKS2 >100 >100 >100 >100 6.5 >100 >100 >100 >100 n.t.
PARP1 >100 >100 n.t. >100 >100 >100 >100 >100 >100 >100
PARP2 >100 >100 >100 27 1.7 38 >100 >100 >100 n.t.
cell-based assayh 1.35 2 n.t. 1.7 1.8 0.59 1.5 1.6 0.95 n.t.
a

Reference (93).

b

Reference (94).

c

Reference (97).

d

Reference (96).

e

Reference (95).

f

In PARP15 gain of binding mutant (Y576L), IC50 = 0.295 μM.

g

n.t. = not tested.

h

Ability of the compounds to rescue HeLa cells from PARP10-induced cell death.