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Antimalarial
Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.- Claudia Alvarez Baron, .et al. , Sci Rep, 2025, Aug 16;15(1):29995 PMID: 40819150
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sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Ella Martin, .et al. , ACS Pharmacol Transl Sci, 2025, May 12;8(9):2996-3006 PMID: 40969890
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Ion channel blocker
Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.- Joe Z.Zhang, .et al. , Cell Stem Cell, 2019, 24, 1-10 PMID: 30880024
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Kir7.1 potassium channels blocker
ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.- Keisuke Obara, .et al. , Journal of Pharmacological Sciences, 2026, 160: 41-50
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Kv1.3 blocker
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
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Potassium Channel Blocker
TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
- Cheong Hoon Seo, .et al. , Transl Res, 2021, Apr 24 PMID: 33905948
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HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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potassium-competitive acid Blocker
TAK-438 is a novel potassium-competitive acid blocker. -
K+/Na+/Ca+ Channel Blocker
Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents. -
Gardos channel blocker
Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM. - Vernakalant is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents.
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NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. - Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
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KATP channel antagonist
Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. - Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
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KCa2.1 channels activator
GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2). -
Potassium Channel activator
Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator. -
Potassium channel blocker
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. - Citronellal or rhodinal or 3,7-dimethyloct-6-en-1-al is a monoterpenoid, the main component in the mixture of terpenoid chemical compounds that give citronella oil its distinctive lemon scent.
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potassium-competitive acid blocker
Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM. - Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
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Peripheral chemoreceptor agonist
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel. -
μ- opioid receptor agonist
Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome. -
K+ Channel inhibitor
K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur). -
Wnt/beta-catenin inhibitor
Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling. -
Kir2 family channels inhibitor
ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5. -
KCNQ2/Q3 potassium channel activator
ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM. -
KCC2 inhibitor
VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). -
HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes. -
mitoKATP channels
BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels. -
KATP activator
Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator. -
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
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potassium channel (non-GIRK1/X) activator
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.

