Discovery and pharmacological profile of new hydrophilic 5-HT4 receptor antagonists
Keywords: 5-HT4 receptor antagonists; hERG; Pharmacokinetic
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Design, synthesis, and biological activities of 1-aryl-1,4-diazepan-2-one derivatives as novel triple reuptake inhibitors
Keywords: XJTZQDVYMGLFOP-YDALLXLXSA-N; CNS; central nervous system; DA; dopamine; 5-HT; serotonin; NE; norepinephrine; DAT; dopamine transporter; SERT; serotonin transporter; NET; norepinephrine transporter; hERG; human ether-a-go-go-related gene K+ channel; TRI; t
Nonsense-mediated mRNA decay due to a CACNA1C splicing mutation in a patient with Brugada syndrome
Keywords: BrS; Brugada syndrome; cDNA; complementary DNA; ECG; electrocardiogram; HEK; human embryo kidney; hERG; human ether-Ã -go-go-related gene; ICa; calcium current; ICD; implantable cardioverter-defibrillator; mRNA; messenger RNA; NMD; nonsense-mediated mRN
Solubility assessment and on-line exposure confirmation in a patch-clamp assay for hERG (human ether-a-go-go-related gene) potassium channel inhibition
Keywords: Exposure; Flow cell; hERG; ICH S7B; Methods; Patch-clamp; Screening; Solubility; Turbidometry; UV spectroscopy;
Insight into the molecular interaction between the cyclic nucleotide-binding homology domain and the eag domain of the hERG channel
Keywords: hERG; Cyclic nucleotide-binding homology domain; KCNH channel; Eag domain; NMR; Ion channel;
In vitro chronic effects on hERG channel caused by the marine biotoxin azaspiracid-2
Keywords: Automated patch clamp; Azaspiracid; Cardiotoxicity; Chronic; hERG; TraffickingAZAs, azaspiracids; AZP, azaspiracid poisoning; BSA, bovine serum albumin; CHO, Chinese hamster ovary; DMSO, dimethyl sulfoxide; DPBS, Dulbecco's phosphate-buffered saline; EC,
Upregulation of functional Kv11.1 isoform expression by inhibition of intronic polyadenylation with antisense morpholino oligonucleotides
Keywords: Potassium channels; hERG; Alternative polyadenylation; Morpholino; Long QT syndrome;
Cardiac Sodium Channel Nav1.5 and Drug-Induced Long QT Syndrome
Keywords: Sodium channel; Nav1.5; Long QT syndrome; Drugs; Arrhythmia; hERG;
Discovery of novel tetrahydroisoquinoline derivatives as orally active N-type calcium channel blockers with high selectivity for hERG potassium channels
Keywords: N-type calcium channel; Pain; hERG;
KV10.1 K+-channel plasma membrane discrete domain partitioning and its functional correlation in neurons
Keywords: PM; plasma membrane; DRM; detergent resistant membrane; Ca-CaM; calcium calmodulin; CaMKII; calcium calmodulin kinase II; HIF; hypoxia inducible factor; SNARE; Soluble NSF Attachment Protein; HERG; human EAG related gene, HEK, human embryonic kidney; GalC
hERG blocking potential of acids and zwitterions characterized by three thresholds for acidity, size and reactivity
Keywords: AZA; acids and zwitterionic ampholytes; DE; donor (electrophilic) superdelocalizability (a.u./eV); DEMaxN; the maximum of DE for all nitrogen atoms in a conformer (a.u./eV); DiamEff; conformer effective cross-sectional diameter, (Ã
); hERG; human ether-a-
A human ether-á-go-go-related (hERG) ion channel atomistic model generated by long supercomputer molecular dynamics simulations and its use in predicting drug cardiotoxicity
Keywords: 1-NP; 1-naphthol; APBS; adaptive Poisson-Boltzmann solver; DBI; Davies-Bouldin index; DMSO; dimethylsulfoxide; EC; extracellular buffer; GAFF; generalized amber force field; hERG; human ether-á-go-go-related K+ ion channel; IC; intracellular buffer;
The role of ubiquitin ligases in cardiac disease
Keywords: AChRs; acetylcholine receptors; AKAP121; A-kinase anchor protein 121; c-Cbl; Casitas b-lineage lymphoma; Cav3; cavelin 3; CHIP; c-terminus of Hsp70-interacting protein; cIAP; cellular inhibitor of apoptosis; cMyBP-C; cardiac myosin binding protein C; Drp1
Ranolazine inhibition of hERG potassium channels: Drug-pore interactions and reduced potency against inactivation mutants
Keywords: Antiarrhythmic; Docking; hERG; Lidocaine; QT interval; Ranolazine;
A novel assessment of nefazodone-induced hERG inhibition by electrophysiological and stereochemical method
Keywords: Nefazodone; hERG; Patch clamp; Cardiotoxicity; HEK-293 cells;
Antisense oligonucleotides on neurobehavior, respiratory, and cardiovascular function, and hERG channel current studies
Keywords: ASO; Antisense Oligonucleotide; CNS; Central Nervous System; ECG; Electrocardiography; FOB; Functional Observatory Battery; GLP; Good Laboratory Practice; hERG; Human Ether-a-go-go related gene; ICH; International Conference on Harmonisation; IC50; The ha
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa
Keywords: NBTI; novel bacterial type II topoisomerase inhibitor; QRDR; quinolone-resistance determining region; hERG; the potassium ion channel encoded by the 'human Ether-a-go-go-Related Gene'; LHS; bicyclic aromatic left-hand side; RHS; aromatic right-hand si
Discovery and optimization of novel small-molecule HIV-1 entry inhibitors using field-based virtual screening and bioisosteric replacement
Keywords: ADME; absorption, distribution, metabolism, and excretion; AMLV; amphotropic murine leukemia virus; BBB; blood-brain barrier; BIF; bioisostere factor; CNS; central nervous system; DCM; dichloromethane; DiEA; diisopropylethylamine; DIPEA; N,N-diisopropyl
Delayed pharyngeal repolarization promotes abnormal calcium buildup in aging muscle
Keywords: N2; bristol strain; MPS-4; MiRP K+ channel accessory subunit 4; EXP-2; expulsion defective defecation 2; HERG; human ether-a-go-go-related-gene; LQTs; long QT syndrome; DAD; delayed afterdepolarization; <APd>; mean action potential duration; <APi>; mean a
Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists
Keywords: CCR1; Antagonists; Chemokines; hERG; Spirocyclic;
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors
Keywords: ERK; extracellular signal-regulated kinase; hERG; human ether-a-go-go related gene; HPCD; 2-hydroxypropyl-β-cyclodextrin; LYSA; lyophilized solubility assay; MEK; mitogen-activated protein kinase; PAMPA; parallel artificial membrane permeability assay; P
A public-private consortium advances cardiac safety evaluation: Achievements of the HESI Cardiac Safety Technical Committee
Keywords: ADRs; adverse drug reactions; CDER; Center for Drug Evaluation and Research; cTn; cardiac troponin; CV; cardiovascular; EMA; European Medicines Agency; EWG; Expert Working Group; ECG; electrocardiogram; HESI; Health and Environmental Sciences Institute; h
The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease
Keywords: Alzheimer's disease; Oxadiazepine; Amyloid precursor protein; Gamma secretase modulator; hERG;
Assessment of beating parameters in human induced pluripotent stem cells enables quantitative in vitro screening for cardiotoxicity
Keywords: iPSC; induced pluripotent stem cell; BMC; benchmark concentration; DMSO; dimethyl sulfoxide; AUC; area under the curve; EC50; effective concentration at 50% of the maximum response; iPSC; Calcium flux; Cardiotoxicity; hERG; Phenotypic screening; Predictiv
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: Comparison of hERG binding and target residence time with PF-3893787
Keywords: Histamine H4 receptor; GPCR; Pyrido[3,2-d]pyrimidine; hERG; Residence time; PF-3893787;
Identification of diterpene alkaloids from Aconitum napellus subsp. firmum and GIRK channel activities of some Aconitum alkaloids
Keywords: Aconitum napellus L. subsp. firmum; Diterpene alkaloids; GIRK; hERG; Cardiovascular ion channels;
Evaluation of an in silico cardiac safety assay: Using ion channel screening data to predict QT interval changes in the rabbit ventricular wedge
Keywords: AP (D); Action Potential (Duration); ECG; electrocardiogram; ECVAM; European Centre for the Validation of Alternative Methods; FLIPR; FLuorescence Imaging Plate Reader; GSK; GlaxoSmithKline; hERG; human-Ether-a-go-go Related Gene; IC50; Concentration for
Hydroxypropyl-β-cyclodextrin impacts renal and systemic hemodynamics in the anesthetized dog
Keywords: CD; cyclodextrin; CI; confidence interval; CO; cardiac output; CV; cardiovascular; DBP; diastolic blood pressure; FDA; Food and Drug Administration; GFR; glomerular filtration rate; GLP; Good Laboratory Practice; hERG; human ether-a-go-go related gene; HP
Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist
Keywords: Bioavailability; hERG; 5-HT4 antagonist; Hydrophilic; Pharmacokinetic; Prodrug;
Arsenic trioxide-induced hERG K+ channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression
Keywords: As2O3; Matrine; Oxymatrine; hERG; Sp1;
A history of the role of the hERG channel in cardiac risk assessment
Keywords: hERG; human ether-a-go-go-related gene; TdP; torsades de pointes; TQT; thorough QT trial; Agonists; Blockers; hERG; Methods; Modeling; Patch clamp; Trafficking;
Anti-addiction drug ibogaine inhibits voltage-gated ionic currents: A study to assess the drug's cardiac ion channel profile
Keywords: hERG; human Ether-Ã -go-go-Related Gene; 18-MC; 18-Methoxycoronaridine; AP; action potential; Anti-addiction drug; hERG potassium channels; Ibogaine; 18-Methoxycoronaridine; QT interval prolongation; Voltage-gated ion channels;
Novel triple reuptake inhibitors with low risk of CAD associated liabilities: Design, synthesis and biological activities of 4-[(1S)-1-(3,4-dichlorophenyl)-2-methoxyethyl]piperidine and related compounds
Keywords: Monoamine reuptake inhibition; Piperidine compounds; Cationic amphiphilic drug (CAD); CYP2D6; hERG; PLsis; Tail suspension test; Antidepressant;
Are hERG channel blockers also phospholipidosis inducers?
Keywords: hERG; Phospholipidosis; qHTS
α-Lipoic acid protects against arsenic trioxide-induced acute QT prolongation in anesthetized guinea pigs
Keywords: Arsenic trioxide; α-lipoic acid; hERG; IKr; IKs; QT prolongation
Indexing molecules for their hERG liability
Keywords: Computational chemistry; Structure activity relations; hERG; Cardio-toxicity; Iterative Stochastic Elimination (ISE)hERG, human ether-a-go-go-related gene; ISE, Iterative Stochastic Elimination; MCC, Matthews' Correlation Coefficient; EF, enrichment facto
Combining structure- and ligand-based approaches for studies of interactions between different conformations of the hERG K+ channel pore and known ligands
Keywords: hERG; Homology building; Molecular docking; QSAR
Methodological innovations expand the safety pharmacology horizon
Keywords: hERG; Lambeth conventions; Arrhythmia; Safety; ICHS7A; ICH S8
Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H1-antihistamine agents
Keywords: Benzimidazole derivatives; Antihistamine activity; SAR; Anti-PAF activity; hERG
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis
Keywords: CCR5 antagonist; Chemokine receptor; hERG
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity
Keywords: CAOVTUXLXXVRSK-AIPQICINSA-N; CCR2 antagonists; Chemokine receptor; hERG;
A β-tryptase inhibitor with a tropanylamide scaffold to improve in vitro stability and to lower hERG channel binding affinity
Keywords: Serine protease; Asthma; COPD; hERG; Tryptase; Inhibitor; Molecular modeling; Structure based drug design; X-ray; Benzylamine;
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2
Keywords: Melanin concentrating hormone (MCH); Quinazolines; MCHR1 antagonists; hERG; Obesity;
Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4â²-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)
Keywords: Histamine-H3 antagonist; Sleep; Wakefulness; CNS; hERG; Clinical candidate;
Multiparameter exploration of piperazine derivatives as δ-opioid receptor agonists for CNS indications
Keywords: Delta opioid agonist; hERG; Permeability; Microsomal clearance; ADME predictive models;
4-Piperidin-4-ylidenemethyl-benzamides as δ-opioid receptor agonists for CNS indications: Identifying clinical candidates
Keywords: Delta opioid agonist; hERG; P-glycoprotein efflux; Microsomal clearance;
Curcumin inhibits hERG potassium channels in vitro
Keywords: Curcumin; Potassium channel; hERG
Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors
Keywords: c-Met kinase; 3,5-Diamino-7-trifluoroquinoline; hERG; Antitumor activity; Structure–activity relationship (SAR)
A422T mutation in HERG potassium channel retained in ER is rescurable by pharmacologic or molecular chaperones
Keywords: Potassium channel; HERG; Long QT syndrome; Patch clamp; Protein trafficking
Pharmacophore modeling for hERG channel facilitation
Keywords: hERG; human ether-a-go-go-related gene; 3D-QSAR; three-dimensional-quantitative structure activity relationships; V1/2; the half maximal of voltage dependence of activation; IC50; the half maximal concentration for inhibition; EC50; the half maximal conce