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BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC₅₀ of 7.35 (pK_i=7.05), and murine PARP-2 (mPARP-2) with a pIC₅₀ of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.

In kinetic experiments with human PARP-1, BYK204165 exhibits potent and competitive inhibition of enzyme activity, yielding a pK_i value of 7.05.
BYK204165 exhibits low potency of PARP inhibition in C4I cells (pIC₅₀ of 5.75).

BYK204165 is not investigated in vivo because of its short half-time (t_1/2) of 23 min measured at rat microsomes in vitro.

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