Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as18F‐labeled PET tracers. The derivatives were evaluated extensively for their off-target profile at 48... Show moreHerein we report the design and synthesis of a series of highly selective CCR2 antagonists as18F‐labeled PET tracers. The derivatives were evaluated extensively for their off-target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution study, demonstrating a promising profile for further preclinical development. This compound represents the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors. Show less