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Structures of recently reported PLD inhibitors (1–5). Halopemide (1), an atypical antipsychotic agent was shown to be a dual PLD1/2 inhibitor, which spawned optimization campaigns that afforded isoform selective (either PLD1 (2) or PLD2 (3 and 4)) inhibitors, as well as a highly potent dual PLD1/2 inhibitor (5).
