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Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.

Ajmaline (Cardiorythmine) is a class Ia anti-arrhythmic compound that is widely used for the diagnosis of Brugada syndrome and the acute treatment of atrial or ventricular tachycardia. Ajmaline inhibits cardiac Kv1.5 and Kv4.3 channels at therapeutic concentrations.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

Amiodarone hydrochloride (Amiodarone HCl) is an antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Branaplam (LMI 070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

Cloperastine hydrochloride (HT-11 hydrochloride) is a type of flavonoid.

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator that enhances hERG currents by slowing inactivation, promoting activation, reducing inactivation, and shortening atrial and ventricular repolarization in a complex manner.

DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

Sarizotan HCl (EMD 128130 HCl) is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinson's Dyskinesia.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Seridopidine (ACR343) is a modulator of dopaminergic activity that is used as an oral therapy for schizophrenia, Parkinson's disease, and Tourette's syndrome.

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

(Iso)-Landipirdine((Iso)-RO5025181) is a selective and potent 5-HT6R antagonist. (Iso)-Landipirdine has a significant effect on the hERG pharmacophore and can be used to study neurological disorders in the Alzheimer's disease class.

Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.

Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.

INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock.

Naluzotan hydrochloride (PRX 00023 hydrochloride) is a hERG K+ channel blocker with an IC50 value of 3800 nM and is commonly used in the study of anxiety and depression.Naluzotan hydrochloride is also a novel, potent, and selective 5-HT1A agonist, with an IC50 value of about 20 nM and a Ki value of about 5.1 Naluzotan hydrochloride is also a novel, potent and selective 5-HT1A agonist with an IC50 of approximately 20 nM and a Ki of approximately 5.1 nM.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

Rosuvastatin (ZD 4522) is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

O-Nornuciferine reveals distinct in vitro hERG blockages measured in HEK293 cells with the IC50 value of 2.89 uM.

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.

Allocryptopine (Thalictrimine) induces muscle contraction and relaxation in urinary bladder and ileum, respectively.

JNJ-42165279 covalently inactivates the FAAH enzyme but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 (10 μM) exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and

ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

GSK369796 Dihydrochloride (N-tert-butylisoquine),is an anti-malaria drug candidate. is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization(IC50 of 7.5 μM)

CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.

ICA-105574 (ICA) is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. It also modulates activation kinetics of the channel.

Daurisoline ((R,R)-Daurisoline) is a hERG inhibitor. Daurisoline is also an autophagy blocker.

SLU-10482, an antiparasitic agent, effectively reduces C. parvum parasitic load in HCT-8 cells with an EC50 value of 0.07 µM. It exhibits lower affinity for human ether-a-go-go (hERG; Kd = 43 µM) compared to its counterpart, SLU-2633. When administered in vivo at dosages of 5 and 15 mg/kg twice daily, SLU-10482 significantly decreases fecal oocyst counts in mice infected with C. parvum.

Halofantrine hydrochloride is a blocker of delayed rectifier potassium current. Halofantrine hydrochloride also via the inhibition of the human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial agent.

DprE1-IN-1 is a potent, orally active DprE1 inhibitor that demonstrates good hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. It also exhibits effective anti-branched bacilli activity in macrophages, reducing the bacterial load by 1.29 log10 CFU.