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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

hERG ion channel

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (1) Bacterial (2) Calcium Channel (2) CCR (1) CMV (1) Cytochrome P450 (2) DNA/RNA Synthesis (1) EBV (1) GLP Receptor (1) Glucocorticoid Receptor (2) GPR68 (1) HCV Protease (2) Histone Methyltransferase (1) HSV (1) Opioid Receptor (1) P-glycoprotein (1) p38 MAPK (1) Parasite (2) Potassium Channel (8) SARS-CoV (1) Serotonin Transporter (2) Sodium Channel (2)
By Research Areas:	Cancer (1) Cardiovascular Disease (4) Infection (8) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (4)

Inhibitors & Agonists

Screening Libraries

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134494

MS48107 2 Publications Verification	GPR68	Neurological Disease
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .

HY-116838

TAM-16	Bacterial	Infection
TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC₅₀ value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel .

HY-136832

Noribogaine hydrochloride	Serotonin Transporter Potassium Channel Arrestin Opioid Receptor	Cardiovascular Disease Neurological Disease
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC₅₀=50-300 nM) and *hERG* channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .

HY-16915

RPR-260243 1 Publications Verification	Potassium Channel	Cardiovascular Disease
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC₅₀=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-12082A

GSK369796 Dihydrochloride	Potassium Channel Parasite	Infection
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits **hERG potassium ion channel repolarization with an IC₅₀** of 7.5 μM.

HY-131335

p38α inhibitor 2	p38 MAPK	Inflammation/Immunology
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC₅₀ of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC₅₀=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .

HY-119101

AZD-5672 1 Publications Verification	CCR Potassium Channel P-glycoprotein	Inflammation/Immunology
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC₅₀=0.32 nM). AZD-5672 shows moderate activity against the *hERG* ion channel (binding IC₅₀=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC₅₀=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .

HY-12946

BI 653048	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

HY-12946A

BI 653048 phosphate	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

HY-12082

GSK369796	Potassium Channel Parasite	Infection
GSK369796 is an affordable and effective antimalarial and inhibits **hERG potassium ion channel repolarization with an IC₅₀** of 7.5 μM .

HY-156976A

Sulcardine hydrochloride	Calcium Channel Sodium Channel	Cardiovascular Disease
Sulcardine hydrochloride is a multi-ion channel blocker that can reduce I_Na and I_Ca with IC₅₀ values of 26.9 µM and 69.2 µM, respectively. Sulcardine hydrochloride is a potent hNav1.5 channel blocker with a mild inhibitory effect on *hERG* channels. Sulcardine hydrochloride has anti-arrhythmic effects .

HY-156976

Sulcardine	Calcium Channel Sodium Channel	Cardiovascular Disease
Sulcardine is a multi-ion channel blocker that can reduce I_Na and I_Ca with IC₅₀ values of 26.9 µM and 69.2 µM, respectively. Sulcardine is a potent hNav1.5 channel blocker with a mild inhibitory effect on *hERG* channels. Sulcardine has anti-arrhythmic effects .

HY-163590

PRMT5-IN-41	Histone Methyltransferase Potassium Channel	Cancer
PRMT5-IN-41 (compound 130) is a potent and orally active PRMT5 inhibitor. PRMT5-IN-41 inhibits hERG ion channel with IC₅₀ value of 1.36 µM .

HY-170511

GLP-1 receptor agonist 15	GLP Receptor Potassium Channel	Metabolic Disease
GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC₅₀ of 0.74 nM. The IC₅₀ for the *hERG* potassium ion channel is 10.1 μM. GLP-1 receptor agonist 15 can be used for research in the field of diabetes .

HY-103268

(Rac)-AZD3839	Potassium Channel	Neurological Disease
(Rac)-AZD3839 is an orally active beta-amyloid precursor protein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease .

HY-181745

Pks13-IN-3	Bacterial	Infection
Pks13-IN-3 is a furo[2,3-b]isoquinoline derivative and Pks13 inhibitor with an IC₅₀ of 1.12 μM. Pks13-IN-3 reduces inhibition of the *hERG* ion channel. Pks13-IN-3 can be used for the research of tuberculosis .

HY-175804

M2 ion channel blocker-2	SARS-CoV	Infection
M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC₅₀: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .

HY-183269

SERT-IN-5	Serotonin Transporter	Neurological Disease
SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a K_i of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression .

HY-170547A

DNA polymerase-IN-6 formic	HSV CMV EBV DNA/RNA Synthesis	Infection
DNA polymerase-IN-6 formic is an antiviral agent and a DNA polymerase inhibitor. DNA polymerase-IN-6 formic inhibits the replication of HCMV, HSV-1, HSV-2 and EBV. DNA polymerase-IN-6 formic exhibits low cytotoxicity in mammalian cells. DNA polymerase-IN-6 formic can be used in research related to viral infections .

Cat. No.	Product Name

HY-L923

Ion Channel Lead-like Compound Library	9000 compounds
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Ion Channel Lead-like Compound Library

9000 compounds

Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.

MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

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