Advances in receptor chromatography for drug discovery and drug–receptor interaction studies

[Display omitted] •This review summarizes the immobilization methods of receptor chromatography.•The applications of receptor chromatography are discussed.•Future challenges of receptor chromatography and solutions have been expounded. Receptor chromatography involves high-throughput separation and accurate drug screening based on specific drug–receptor recognition and affinity, which has been widely used to screen active compounds in complex samples. This review summarizes the immobilization methods for receptors from three aspects: random covalent immobilization methods, site-specific covalent immobilization methods and dual-target receptor chromatography. Meanwhile, it focuses on its applications from three angles: screening active compounds in natural products, in natural-product-derived DNA-encoded compound libraries and drug–receptor interactions. This review provides new insights for the design and application of receptor chromatography, high-throughput and accurate drug screening, drug–receptor interactions and more.