By means of our fluorescent CCR2 ligand 14, we report the development of the first small molecule-based fluorescent probe targeting the IABS of CCR2. This tool enabled equilibrium as well as kinetic binding studies via the NanoBRET technique. In a displacement setup, 14 was used for the detection of high affinity intracellular CCR2 antagonists as well as for the identification of low molecular weight ligands (fragments). Due to its straightforward homogeneous assay protocol, our membrane-based NanoBRET displacement assay is suitable for high-throughput screening approaches. In addition, we show that 14 can be used as a molecular tool to study cellular target engagement for the IABS of CCR2. Thus, 14 represents a promising tool for future studies targeting the IABS of CCR2.