The pick of the pockets : The first inhibitors for IspD, an enzyme from the non‐mevalonate pathway of isoprenoid biosynthesis, are described. High‐throughput‐screening revealed a hit with an IC50 value of 140 nM . Co‐crystal structure analyses of the binding mode in the newly formed allosteric pocket (see structure, red ball: water O atom), lead to the synthesis of a set of 17 derivatives which were tested to optimize the herbicidal activity.