Drug-induced liver injury (DILI) has been a long-standing concern of modern medicine, and the single most frequent reason for drug nonapprovals and postapproval restrictions or withdrawals. Chemical probes for early diagnosis of DILI has triggered a tremendous interest in the field of molecular imaging. In this review, we make a brief summary of the recently developed chemical probes and their applications in DILI imaging with special attention to the design of chemical probes, mechanism of their actions and their performances in DILI imaging.