Table 6.

Potencies and selectivities of representative and most‐studied K_V1.3 inhibitors from high‐throughput screening approaches

			Potency (nM)
Structural class	Compound	Test type	IC50	K d	Selectivity
Dihydroquinolines	1 145, 146, 149	125I‐charybdotoxin binding to Jurkat T	83	‐	Potently inhibited voltage‐gated neuronal Na+ channels in CHO cells (K i = 9 nM)
	1a 145, 146, 149	lymphocytes (n‐type K+ channels)	‐	120	No selectivity against KV1.4 (IC50 = 300 nM); 60‐ to 270‐fold selectivity against other Kv1 family channels
Piperidines	2 150, 151	86Rb+ efflux in human T cells	400	‐	Potently inhibited KV1.4 (IC50 = 170 nM); 10‐fold selectivity over KV1.2; 40‐fold selectivity over KV3.1
Benzamides	3 152, 153, 154	86Rb+ efflux in CHO cells, expressing KV1.3	200	‐	Inhibited KV1.x family channels with similar potencies (no selectivity)
	3f 152, 153, 154	channels	50	‐	Sixfold selectivity over KV1.x (heteromultimeric KV1.1/KV1.2 channels)
	3g 152, 153, 154		100	‐	No selectivity over KV1.x (heteromultimeric KV1.1/KV1.2 channels)
Triterpenoids	Correolide 4 155, 156, 157, 158	86Rb+ efflux in CHO cells expressing KV1.3 channel	86	‐	Inhibited KV1x family channels with 4‐ to 14‐fold lower potency
	Correolide analog 4a 155, 156, 157, 158	Plasma membranes from CHO/Kv1.3 cells	‐	11