WD2000-012547是一种选择性的PARP-1抑制剂,pKi为8.221。
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WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221.
Poly(ADP-ribose) polymerase-1 (PARP-1) functions as a DNA damage sensor and signaling molecule. It plays a vital role in the repair of DNA strand breaks induced by radiation and chemotherapeutic drugs; inhibitors of this enzyme have the potential to improve cancer chemotherapy or radiotherapy. WD2000-012547 (Compound 66) is a representative PARP-1 inhibitor with a pKi of 8.221[1].
[1]. Fatima S, et al. Multiple receptor conformation docking, dock pose clustering and 3D QSAR studies on human poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. J Recept Signal Transduct Res. 2014 Oct;34(5):417-30.
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