Table 8.

Potencies and selectivities of representative hit compounds from exploitation of biological information approaches

			Potency (nM)
Structural class	Compound	Cell type	IC50	EC50	Selectivity tests
5‐Methoxysoralen	9 170, 171	L929 cells stably expressing KV1.3; manual whole‐cell patch‐clamp	‐	100,000	No selectivity
Psora‐4	9b 170, 171		‐	3	Lacking selectivity over KV1.5 (EC50 = 8 nM), 17‐ to 70‐fold selectivity over Kv1x family channels
PAP‐1	9c 170, 171		‐	2	23‐fold selectivity over KV1.5
Furoquinoline	9d 172	L929 cells expressing KV1.3; whole‐cell patch‐clamp	150	‐	Threefold selectivity over KV1.5
Acridinone	9e 172		165	‐	Threefold selectivity over KV1.5
Furochromene‐7‐thione	9f 172		17	‐	22‐fold selectivity over KV1.5
Clofazimine	10 173, 174	Jurkat T cells	300	‐	Moderate selectivity over KV1.1, KV1.2, KV1.5, and KV3.1 (10 µM: ≤ 50% inhibition)
Diphenoxylate	11 175	L929 cells expressing KV1.3; manual whole‐cell patch‐clamp	5000	‐	Not tested
Diphenoxylate analog	11a 175		750	‐