Table 5.

Strategies for the discovery of small‐molecule K_V1.3 inhibitors

Strategy	Assay	Compound
High‐throughput screening	Ligand binding assays	1
	Ion flux 86Rb assays	2–4
	Automated electrophysiological assays	5–8
Exploitation of biological information	Folk medicine; ethnopharmacology	9, 9a–9f
	Drug repurposing	10 (clofazimine)
	Clinical observations of side effects	11 (diphenoxylate)
Structure‐based drug design methodology	Computer‐aided drug design—virtual screening	12, 13
Ligand‐based drug design methodology	Computer‐aided ligand‐based three‐dimensional similarity searches	14, 15
	Analogs of natural plant compounds	16a–16f
	Peptidomimetics—synthetic ligands of peptide toxins	17–20