Ligand–receptor interactions triggering signal transduction components of many sensory pathways, remain elusive due to paucity of high-throughput screening methods. Here we describe our use of small molecule microarrays comprising of small glycans, amino and organic acids, salts, and other known chemoeffectors, for screening of ligands specific to various sensory receptors, followed by surface plasmon resonance to verify the veracity and to determine the affinity constants of the interactions. This methodology allows for rapid and identification of the direct ligand binding between the sensory receptors and their specific ligands.