Tolazamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2; IC50 = 4.2 µM in HEK293 cells transfected with the human receptor).

The first small-molecule inhibitor of renal outer medullary potassium channel (ROMK, Kir1.1) and Kir7.1 with IC50 of 294 nM for ROMK.

RPR260243 was the first reported hERG channel activator.

Nimodipine(Nimotop) is a dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity.Nimodipine decreases intracellular free Ca2+,Beclin-1 and autophagy.

Nicorandil is potassium channel activator.

Inhibitor of ATP-sensitive K+ channel activity in MIN 6 cells. Has also been shown to bind sulfonylurea receptors as well.

IK1 inhibitor PA-6 is an efficient, specific inhibitor of inward rectifier current (IK1), blocks KIR2.x currents of human and mouse with IC50 of 12-15 nM.

Flupirtine maleateis a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection. Currently under a clinical trial (recruiting phase) as a treatment for Multiple Sclerosis and has been used as an analgesic.

Dronedarone is a Class III antiarrhythmic and a multi-channel blocker for atrial fibrillation. It blocks potassium and sodium and is a calcium channel protein inhibitor.

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).

Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK).

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK) with IC50 of 0.25 nM.

A selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 8 uM in T1+ flux assays, does not inhibit Kir7.1 at 100 uM.

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A potent, selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays.

A potent Kir7.1 inhibitor with IC50 of 2.0 uM, induces long-lasting uterine contractility similar to those observed with VU590..

A potent inwardly rectifying K+ channel Kir7.1 inhibitor with IC50 of 5.6 uM in T1+ flux assays.

A novel specific, cell permeant modulator of Kv3 channels with EC50 of 0.9 and 1.9 uM for Kv3.1b and Kv3.2a, respectively.

A novel selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A imidazoline compound that stimulate insulin release by inhibition of ATP-dependent K+ channels and inducing of Ca2+ mobilization in mouse pancreatic beta-cells.