ML323 exerts a selective and reversible effect on the catalytic activity of USP1 in an allosteric manner that misaligns the conformation of Ub‐binding motif.[274] Unexpectedly, ML323 enhances cisplatin susceptibility in osteosarcoma and NSCLC cells through affecting the DNA damage response.[274] Moreover, GW7647 and pimozide also restrain USP1 catalytic activity in a non‐selective way. The gene discussed is USP1; the disease is non-small cell lung carcinoma.