The biogenesis and metabolism of RNAs are mediated by extensive interactions with RNA-binding proteins, regulating various biological processes and cellular activities. Dysregulations of the pervasive RNA–protein interactions are closely associated with or can lead to a wide range of human diseases. Subsequently, both RNA-binding proteins and disease-associated RNAs are appealing targets for the development of small molecules as chemical biological probes and therapeutic candidates. In this context, the overall goal of my group is to develop small-molecule binders and modulators, as well as derived proximity-inducing bifunctional molecules, targeting RNA-binding proteins of different species using a combination of multifaceted approaches covering screening and rational design methods. Herein, I will present our results in the identification of such molecules targeting three particular classes of RNA-binding proteins: the miRNA-binding protein LIN28, the single-stranded RNA-cleaving ribonuclease RNase L, and mRNA-modifying proteins involved in m6A-methylation.